EA200100061A1 - Производные фталазина в качестве ингибиторов фосфодиэстеразы 4 - Google Patents
Производные фталазина в качестве ингибиторов фосфодиэстеразы 4Info
- 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
Links
Classifications
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
-
- 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
- C07D405/06—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 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.
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)
Publication number | Priority date | Publication date | Assignee | Title |
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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)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
-
1998
- 1998-07-21 IT IT98MI001671A patent/ITMI981671A1/it unknown
-
1999
- 1999-07-16 JP JP2000561175A patent/JP2002521371A/ja active Pending
- 1999-07-16 CA CA002337954A patent/CA2337954A1/en not_active Abandoned
- 1999-07-16 EP EP99932894A patent/EP1098886A1/en not_active Withdrawn
- 1999-07-16 EA EA200100061A patent/EA003702B1/ru not_active IP Right Cessation
- 1999-07-16 HU HU0103349A patent/HUP0103349A3/hu unknown
- 1999-07-16 NZ NZ507930A patent/NZ507930A/xx unknown
- 1999-07-16 IL IL13949199A patent/IL139491A0/xx unknown
- 1999-07-16 US US09/764,983 patent/US6340684B1/en not_active Expired - Fee Related
- 1999-07-16 WO PCT/EP1999/005068 patent/WO2000005219A1/en not_active Application Discontinuation
- 1999-07-16 CZ CZ2001240A patent/CZ2001240A3/cs unknown
- 1999-07-16 AU AU49116/99A patent/AU766076B2/en not_active Ceased
-
2000
- 2000-11-13 ZA ZA200006577A patent/ZA200006577B/xx unknown
-
2001
- 2001-11-14 US US09/987,266 patent/US6498160B2/en not_active Expired - Fee Related
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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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ KZ KG MD TJ TM |
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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) |
Designated state(s): BY RU |