EA200100061A1 - Производные фталазина в качестве ингибиторов фосфодиэстеразы 4 - Google Patents

Производные фталазина в качестве ингибиторов фосфодиэстеразы 4

Info

Publication number
EA200100061A1
EA200100061A1 EA200100061A EA200100061A EA200100061A1 EA 200100061 A1 EA200100061 A1 EA 200100061A1 EA 200100061 A EA200100061 A EA 200100061A EA 200100061 A EA200100061 A EA 200100061A EA 200100061 A1 EA200100061 A1 EA 200100061A1
Authority
EA
Eurasian Patent Office
Prior art keywords
aryl
alkyl
heterocycle
group
optionally substituted
Prior art date
Application number
EA200100061A
Other languages
English (en)
Other versions
EA003702B1 (ru
Inventor
Мауро Наполетано
Габриеле Норчини
Джанкарло Гранчини
Франко Пеллачини
Габриеле Мораццони
Original Assignee
Дзамбон Гроуп С.П.А.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Дзамбон Гроуп С.П.А. filed Critical Дзамбон Гроуп С.П.А.
Publication of EA200100061A1 publication Critical patent/EA200100061A1/ru
Publication of EA003702B1 publication Critical patent/EA003702B1/ru

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Classifications

    • 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
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30Phthalazines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30Phthalazines
    • C07D237/32Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30Phthalazines
    • C07D237/34Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

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

Abstract

Соединения формулы (I), где B представляет NH, метилен, Cалкиленовую цепь, необязательно разветвленную, и/или ненасыщенную, и/или прерванную Cциклоалкильным остатком; A представляет фенил или гетероцикл, необязательно замещенный; R представляет два атома водорода или C=O группу, когдапредставляет одинарную связь, или, когдапредставляет двойную связь, R представляет водород, необязательно замещенный арил или гетероцикл, (C)-алкил, (C)-алкенил или (C)-алкинил, необязательно замещенный арилом или гетероциклом; арилокси, гетероциклилокси, арил-C-алкокси, гетероциклил-C-алкокси, аминогруппу, замещенную одной или двумя Cалкильной(ыми) группой(ами), ариламино, гетероциклиламино, арил-C-алкиламино, гетероциклил-C-алкиламино; Rпредставляет C-алкил, арил, арил-C-алкил, C-циклоалкильную группу, необязательно содержащую атом кислорода и/или замещенную; Rпредставляет C-алкил; полифтор-C-алкильную группу; R, когдапредставляет одинарную связь, представляет (a) водород; (b) C-алкил, необязательно замещенный арилом, гетероциклом или CORгруппой, где Rпредставляет гидрокси, C-алкокси или гидроксиамино; (c) -COR, где Rпредставляет водород, арил, арил-C-алкил, аминогруппу, необязательно алкилированную или моногидроксилированную, гидрокси, C-алкокси, карбокси, C-алкоксикарбонил, формулу|HN=c-NH(II)или C-алкил, необязательно замещенный гетероциклом; d) C-алкилсульфонил; N→O производные соединений формулы (I) и их фармацевтически приемлемые соли; являются ингибиторами PDE 4.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200100061A 1998-07-21 1999-07-16 Производные фталазина в качестве ингибиторов фосфодиэстеразы 4 EA003702B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT98MI001671A ITMI981671A1 (it) 1998-07-21 1998-07-21 Derivati ftalazinici inibitori della fosfodisterasi 4
PCT/EP1999/005068 WO2000005219A1 (en) 1998-07-21 1999-07-16 Phthalazine derivatives as phosphodiesterase 4 inhibitors

Publications (2)

Publication Number Publication Date
EA200100061A1 true EA200100061A1 (ru) 2001-08-27
EA003702B1 EA003702B1 (ru) 2003-08-28

Family

ID=11380475

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100061A EA003702B1 (ru) 1998-07-21 1999-07-16 Производные фталазина в качестве ингибиторов фосфодиэстеразы 4

Country Status (13)

Country Link
US (2) US6340684B1 (ru)
EP (1) EP1098886A1 (ru)
JP (1) JP2002521371A (ru)
AU (1) AU766076B2 (ru)
CA (1) CA2337954A1 (ru)
CZ (1) CZ2001240A3 (ru)
EA (1) EA003702B1 (ru)
HU (1) HUP0103349A3 (ru)
IL (1) IL139491A0 (ru)
IT (1) ITMI981671A1 (ru)
NZ (1) NZ507930A (ru)
WO (1) WO2000005219A1 (ru)
ZA (1) ZA200006577B (ru)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1296984B1 (it) * 1997-12-19 1999-08-03 Zambon Spa Derivati ftalazinici inibitori della fosfodiesterasi 4
ITMI981671A1 (it) 1998-07-21 2000-01-21 Zambon Spa Derivati ftalazinici inibitori della fosfodisterasi 4
DE19921567A1 (de) 1999-05-11 2000-11-16 Basf Ag Verwendung von Phthalazine-Derivaten
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
DE19963607B4 (de) * 1999-12-23 2005-12-15 Schering Ag Verfahren zur Herstellung von 4-(Heteroaryl-methyl) halogen-1(2H)-phthalazinonen
ITMI20000261A1 (it) 2000-02-16 2001-08-16 Zambon Group Processo per la preparazione di piridiniliden-ftalidi
US7151102B2 (en) * 2000-10-30 2006-12-19 Kudos Pharmaceuticals Limited Phthalazinone derivatives
US7196085B2 (en) 2002-04-30 2007-03-27 Kudos Pharmaceuticals Limited Phthalazinone derivatives
GB0305681D0 (en) 2003-03-12 2003-04-16 Kudos Pharm Ltd Phthalazinone derivatives
US7449464B2 (en) 2003-03-12 2008-11-11 Kudos Pharmaceuticals Limited Phthalazinone derivatives
EP1745039A4 (en) * 2004-05-08 2009-07-22 Neurogen Corp 3-ARYL-5,6-DISUBSTITUTED PYRIDAZINES
ES2257152B1 (es) * 2004-05-31 2007-07-01 Laboratorios Almirall S.A. Combinaciones que comprenden agentes antimuscarinicos y agonistas beta-adrenergicos.
GB0419072D0 (en) 2004-08-26 2004-09-29 Kudos Pharm Ltd Phthalazinone derivatives
AU2005282721A1 (en) * 2004-09-03 2006-03-16 Memory Pharmaceuticals Corporation 4-substituted 4, 6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms
AR050948A1 (es) 2004-09-24 2006-12-06 Hoffmann La Roche Derivados de ftalazinona; su obtencion y su utilizacion en la fabricacion de medicamentos para el tratamiento del cancer.
GB0428111D0 (en) * 2004-12-22 2005-01-26 Kudos Pharm Ltd Pthalazinone derivatives
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
GB0521373D0 (en) 2005-10-20 2005-11-30 Kudos Pharm Ltd Pthalazinone derivatives
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
EP1991531A1 (en) * 2006-02-28 2008-11-19 Amgen Inc. Cinnoline and quinoxaline derivates as phosphodiesterase 10 inhibitors
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
MX2008014320A (es) 2006-05-09 2009-03-25 Braincells Inc Neurogenesis mediada por el receptor de 5-hidroxitriptamina.
CN101500997A (zh) * 2006-06-15 2009-08-05 库多斯药物有限公司 Parp抑制剂
JP2009539962A (ja) * 2006-06-15 2009-11-19 クドス ファーマシューティカルズ リミテッド Parp阻害剤としての2−オキシヘテロアリールアミド誘導体
CN101484421A (zh) * 2006-06-15 2009-07-15 库多斯药物有限公司 作为parp抑制剂的2-氧基苯甲酰胺衍生物
MX2009002496A (es) 2006-09-08 2009-07-10 Braincells Inc Combinaciones que contienen un derivado de 4-acilaminopiridina.
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
US20080280910A1 (en) * 2007-03-22 2008-11-13 Keith Allan Menear Phthalazinone derivatives
TW200900396A (en) * 2007-04-10 2009-01-01 Kudos Pharm Ltd Phthalazinone derivatives
US20090023727A1 (en) * 2007-07-05 2009-01-22 Muhammad Hashim Javaid Phthalazinone derivatives
US7981890B2 (en) 2007-09-14 2011-07-19 Astrazeneca Ab Phthalazinone derivatives
BRPI0817537B1 (pt) * 2007-10-17 2022-04-05 Kudos Pharmaceuticals Limited 4-[3-(4-ciclopropanocarbonil-piperazina-1-carbonil)-4-fluoro-benzil]-2h-ftalazin-1-ona, método para obtê-lo, composição farmacêutica compreendendo o mesmo, bem como usos terapêuticos do dito composto
UY31603A1 (es) 2008-01-23 2009-08-31 Derivados de ftalazinona
EP2100599A1 (en) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
EP2100598A1 (en) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
HRP20161154T4 (hr) * 2008-10-07 2023-09-29 Kudos Pharmaceuticals Limited Farmaceutska formulacija 514
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
TW201114756A (en) * 2009-07-15 2011-05-01 Astrazeneca Ab Phthalazinone compound
EP2510928A1 (en) 2011-04-15 2012-10-17 Almirall, S.A. Aclidinium for use in improving the quality of sleep in respiratory patients
EP2804603A1 (en) 2012-01-10 2014-11-26 President and Fellows of Harvard College Beta-cell replication promoting compounds and methods of their use
US9783529B2 (en) 2013-03-13 2017-10-10 Flatley Discovery Lab, Llc Pyridazinone compounds and methods for the treatment of cystic fibrosis

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3274185A (en) * 1963-10-08 1966-09-20 S E Massengill Company Phthalazine derivatives
GB2063249A (en) * 1979-10-09 1981-06-03 Mitsubishi Yuka Pharma 4-Phenylphthalazine derivatives
US6207666B1 (en) * 1995-06-07 2001-03-27 Cell Pathways, Inc. Method for treating a patient having precancerous lesion with 4-phenylphthalazine derivatives
DE69720515T2 (de) * 1996-12-18 2004-02-19 Neurogen Corp., Branford Isoquinolinamin und phtalazinamin derivate, die reagieren mit crf rezeptoren
IT1296985B1 (it) 1997-12-19 1999-08-03 Zambon Spa Derivati benzazinici inibitori della fosfodiesterasi 4
IT1296984B1 (it) * 1997-12-19 1999-08-03 Zambon Spa Derivati ftalazinici inibitori della fosfodiesterasi 4
ITMI981670A1 (it) 1998-07-21 2000-01-21 Zambon Spa Derivati ftalazinici inibitori della fosfodiesterasi 4
ITMI981671A1 (it) 1998-07-21 2000-01-21 Zambon Spa Derivati ftalazinici inibitori della fosfodisterasi 4

Also Published As

Publication number Publication date
HUP0103349A2 (hu) 2002-02-28
HUP0103349A3 (en) 2003-01-28
ZA200006577B (en) 2002-04-24
WO2000005219A1 (en) 2000-02-03
EA003702B1 (ru) 2003-08-28
US20020058662A1 (en) 2002-05-16
ITMI981671A1 (it) 2000-01-21
EP1098886A1 (en) 2001-05-16
AU4911699A (en) 2000-02-14
CZ2001240A3 (cs) 2001-09-12
CA2337954A1 (en) 2000-02-03
US6498160B2 (en) 2002-12-24
NZ507930A (en) 2002-11-26
AU766076B2 (en) 2003-10-09
ITMI981671A0 (it) 1998-07-21
US6340684B1 (en) 2002-01-22
JP2002521371A (ja) 2002-07-16
IL139491A0 (en) 2001-11-25

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