[go: up one dir, main page]

PE20061129A1 - Derivados de purina como agonistas del receptor de adenosina a2a - Google Patents

Derivados de purina como agonistas del receptor de adenosina a2a

Info

Publication number
PE20061129A1
PE20061129A1 PE2005001232A PE2005001232A PE20061129A1 PE 20061129 A1 PE20061129 A1 PE 20061129A1 PE 2005001232 A PE2005001232 A PE 2005001232A PE 2005001232 A PE2005001232 A PE 2005001232A PE 20061129 A1 PE20061129 A1 PE 20061129A1
Authority
PE
Peru
Prior art keywords
amino
adenosine
agonists
cyclopentil
purin
Prior art date
Application number
PE2005001232A
Other languages
English (en)
Inventor
Robin Alec Fairhurst
Roger John Taylor
Original Assignee
Novartis Ag
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
Priority claimed from GB0423551A external-priority patent/GB0423551D0/en
Priority claimed from GB0514619A external-priority patent/GB0514619D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20061129A1 publication Critical patent/PE20061129A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/40Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6

Landscapes

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

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE R1 ES H, ALQUILO(C1-C8), CICLOALQUILO(C3-C8), ARALQUILO(C7-C14), ENTRE OTROS; R2 ES H O ALQUILO(C1-C8) OPCIONALMENTE SUSTITUIDO CON ARILO(C6-C10); R3 ES H, HALOGENO, ALQUENILO(C2-C8), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: TRIFLUOROACETATO DE N-[(1S,2R,3S,4R)-4-(6-AMINO-2-CLORO-PURIN-9-IL)-2,3-DIHIDROXI-CICLOPENTIL]-METAN-SULFONAMIDA, TRIFLUOROACETATO DE N-[(1S,2R,3S,4R)-4-(6-AMINO-2-FENETIL-AMINO-PURIN-9-IL)-2,3-DIHIDROXI-CICLOPENTIL]-PROPIONAMIDA, TRIFLUOROACETATO DE N-[(1S,2R,3S,4R)-4-(6-AMINO-2-HEX-1-INIL-PURIN-9-IL)-2,3-DIHIDROXI-CICLOPENTIL]-PROPIONAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON AGONISTAS DEL RECEPTOR DE ADENOSINA A2A SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA, BRONQUITIS CRONICA, ENFISEMA, ASMA
PE2005001232A 2004-10-22 2005-10-20 Derivados de purina como agonistas del receptor de adenosina a2a PE20061129A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0423551A GB0423551D0 (en) 2004-10-22 2004-10-22 Organic compounds
GB0514619A GB0514619D0 (en) 2005-07-15 2005-07-15 Organic compounds

Publications (1)

Publication Number Publication Date
PE20061129A1 true PE20061129A1 (es) 2006-12-13

Family

ID=35589070

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2005001232A PE20061129A1 (es) 2004-10-22 2005-10-20 Derivados de purina como agonistas del receptor de adenosina a2a
PE2010000097A PE20100266A1 (es) 2004-10-22 2005-10-20 Derivados de purina como agonistas del receptor de adenosina a2a

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2010000097A PE20100266A1 (es) 2004-10-22 2005-10-20 Derivados de purina como agonistas del receptor de adenosina a2a

Country Status (21)

Country Link
US (1) US8163754B2 (es)
EP (2) EP1805181B1 (es)
JP (1) JP4904279B2 (es)
KR (1) KR20070073798A (es)
AR (1) AR051642A1 (es)
AU (2) AU2005298878B2 (es)
BR (1) BRPI0517455A (es)
CA (1) CA2582434A1 (es)
EC (1) ECSP077404A (es)
ES (1) ES2394453T3 (es)
GT (1) GT200500281A (es)
IL (1) IL182528A0 (es)
MA (1) MA28931B1 (es)
MX (1) MX2007004735A (es)
NO (1) NO20072122L (es)
NZ (1) NZ554546A (es)
PE (2) PE20061129A1 (es)
RU (1) RU2403253C2 (es)
TN (1) TNSN07154A1 (es)
TW (1) TW200630366A (es)
WO (1) WO2006045552A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GT200500281A (es) 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
GB0500785D0 (en) 2005-01-14 2005-02-23 Novartis Ag Organic compounds
GB0607948D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607953D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
RU2457209C2 (ru) * 2006-04-21 2012-07-27 Новартис Аг Производные пурина, предназначенные для применения в качестве агонистов аденозинового рецептора а2а
GB0607945D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607954D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607944D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
EP1889846A1 (en) * 2006-07-13 2008-02-20 Novartis AG Purine derivatives as A2a agonists
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
KR20090087054A (ko) * 2006-11-10 2009-08-14 노파르티스 아게 시클로펜텐 디올 모노아세테이트 유도체
TW200837055A (en) * 2007-03-13 2008-09-16 Arete Therapeutics Inc Soluble epoxide hydrolase inhibitors
JP2011500631A (ja) * 2007-10-17 2011-01-06 ノバルティス アーゲー アデノシンa1受容体リガンドとしてのプリン誘導体
US20090181934A1 (en) * 2007-10-17 2009-07-16 Novartis Ag Organic Compounds
KR20120107065A (ko) 2009-06-30 2012-09-28 포레스트 래보러토리즈 홀딩스 리미티드 A2ar 효현제용 알콕시 카르보닐 아미노 알키닐 아데노신 화합물 및 그 유도체
EP3039126B1 (en) 2013-08-26 2019-10-09 The J. David Gladstone Institutes, A Testamentary Trust Established under The Will of J. David Gladstone Small molecule cellular reprogramming to generate neuronal cells

Family Cites Families (194)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
GB1528382A (en) 1974-12-26 1978-10-11 Teijin Ltd Cyclopentene diols and acyl esters thereof and processes for their preparation
JPS5481295A (en) * 1977-12-13 1979-06-28 Suami T Adenosin analogue compounds
FR2459240A1 (fr) 1979-06-21 1981-01-09 Cm Ind Aminopiperidines anorexigenes, procede pour leur preparation, intermediaires dans ledit procede et medicaments qui les contiennent
EP0147716A3 (de) 1983-12-24 1987-10-28 ANT Nachrichtentechnik GmbH Verfahren und Anordnung zur verschlüsselbaren Übertragung einer Nachrichten-Binärzeichenfolge mit Authentizitätsprüfung
JPS6235216A (ja) 1985-08-09 1987-02-16 Noritoshi Nakabachi 不均質物質層の層厚非破壊測定方法および装置
US4738954A (en) 1985-11-06 1988-04-19 Warner-Lambert Company Novel N6 -substituted-5'-oxidized adenosine analogs
US4873360A (en) 1986-07-10 1989-10-10 Board Of Governors Of Wayne State University Process for the preparation of cyclopentanoids and novel intermediates produced thereby
EP0267878A1 (en) 1986-11-14 1988-05-18 Ciba-Geigy Ag N9-cyclopentyl-substituted adenine derivatives
US4954504A (en) 1986-11-14 1990-09-04 Ciba-Geigy Corporation N9 -cyclopentyl-substituted adenine derivatives having adenosine-2 receptor stimulating activity
JP2586897B2 (ja) 1987-03-09 1997-03-05 富士薬品工業株式会社 光学活性なシス−シクロペンテン−3,5−ジオ−ルモノエステルの製造法
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
DE69123974T2 (de) 1990-09-25 1997-05-07 Rhone-Poulenc Rorer International (Holdings) Inc., Greenville, Del. Verbindungen welche antihypertensive und antiischemische eigenschaften besitzen
US5561134A (en) * 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
WO1993018007A1 (fr) 1992-03-13 1993-09-16 Tokyo Tanabe Company Limited Nouveau derive de carbostyrile
DE69331265T2 (de) 1992-04-02 2002-08-08 Smithkline Beecham Corp., Philadelphia Verbindungen zur behandlung von entzündlichen erkrankungen und zur hemmung der produktion von tumornekrosefaktor
JP3192424B2 (ja) 1992-04-02 2001-07-30 スミスクライン・ビーチャム・コーポレイション アレルギーまたは炎症疾患の治療用化合物
EP0633776B1 (en) 1992-04-02 2001-05-09 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
IT1254915B (it) 1992-04-24 1995-10-11 Gloria Cristalli Derivati di adenosina ad attivita' a2 agonista
US5688774A (en) 1993-07-13 1997-11-18 The United States Of America As Represented By The Department Of Health And Human Services A3 adenosine receptor agonists
US5691188A (en) 1994-02-14 1997-11-25 American Cyanamid Company Transformed yeast cells expressing heterologous G-protein coupled receptor
US6143749A (en) * 1995-06-07 2000-11-07 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
AP772A (en) 1996-01-02 1999-10-15 Aventis Pharma Inc Process for preparing 2,4-dihydroxypyridine and 2,4-dihydroxy-3-nitropyridine.
US6376472B1 (en) 1996-07-08 2002-04-23 Aventis Pharmaceuticals, Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
WO1998050047A1 (en) 1997-05-09 1998-11-12 Trustees Of The University Of Pennsylvania Methods and compositions for reducing ischemic injury of the heart by administering adenosine receptor agonists and antagonists
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
FR2780057B1 (fr) 1998-06-18 2002-09-13 Sanofi Sa Phenoxypropanolamines, procede pour leur preparation et compositions pharmaceutiques les contenant
AU750462B2 (en) 1998-06-23 2002-07-18 Glaxo Group Limited 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
GB9813535D0 (en) * 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813540D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813554D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
WO2000000531A1 (en) 1998-06-30 2000-01-06 The Dow Chemical Company Polymer polyols and a process for the production thereof
ATE331726T1 (de) 1998-10-16 2006-07-15 Pfizer Adenine-derivate
ES2228163T3 (es) 1998-12-31 2005-04-01 Aventis Pharmaceuticals Inc. Procedimiento para preparar derivados de desaza-adenosina n6-sustituidos.
US7427606B2 (en) 1999-02-01 2008-09-23 University Of Virginia Patent Foundation Method to reduce inflammatory response in transplanted tissue
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
CZ20013940A3 (cs) 1999-05-04 2002-04-17 Schering Corporation Piperazinové deriváty uľitečné jako CCR5 antagonisté
EP1659111A3 (en) 1999-05-04 2007-05-09 Schering Corporation Piperidine derivatives useful as ccr5 antagonists
US6683115B2 (en) 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
US6322771B1 (en) 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
US6403567B1 (en) 1999-06-22 2002-06-11 Cv Therapeutics, Inc. N-pyrazole A2A adenosine receptor agonists
US6214807B1 (en) 1999-06-22 2001-04-10 Cv Therapeutics, Inc. C-pyrazole 2A A receptor agonists
NZ516260A (en) * 1999-07-02 2004-08-27 Eisai Co Ltd Fused imidazole compounds and remedies for diabetes mellitus
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
SK287231B6 (sk) 1999-08-21 2010-04-07 Nycomed Gmbh Liečivo zahŕňajúce PDE inhibítor a agonistu beta2 adrenoreceptora
US6586413B2 (en) 1999-11-05 2003-07-01 The United States Of America As Represented By The Department Of Health And Human Services Methods and compositions for reducing ischemic injury of the heart by administering adenosine receptor agonists and antagonists
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
NZ522677A (en) 2000-04-27 2004-10-29 Boehringer Ingelheim Pharma Novel, slow-acting betamimetics, a method for their production and their use as medicaments
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
DK1300407T4 (da) 2000-06-27 2011-09-05 S A L V A T Lab Sa Carbamater afledt af arylalkylaminer
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
ATE416184T1 (de) 2000-08-05 2008-12-15 Glaxo Group Ltd 17.beta.-carbothioat 17.alpha.- arylkarbonyloxyloxy androstanderivate als anti- phlogistische medikamente
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
HUP0303529A3 (en) 2000-12-22 2008-03-28 Almirall Ag New quinuclidine carbamate derivatives, process for their preparation and pharmaceutical compositions containing them and their use
SK287414B6 (sk) 2000-12-28 2010-09-07 Laboratorios Almirall, S.A. Chinuklidínové deriváty a kompozície s ich obsahom
ATE292973T1 (de) 2001-01-16 2005-04-15 Can Fite Biopharma Ltd Verwendung eines adenosin-a3-rezeptor-agonisten zur hemmung der virenreplikation
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
GB2372741A (en) 2001-03-03 2002-09-04 Univ Leiden C2,8-Disubstituted adenosine derivatives and their different uses
ES2288543T3 (es) 2001-03-08 2008-01-16 Glaxo Group Limited Agonistas de beta-adrenorreceptores.
US20040162422A1 (en) * 2001-03-20 2004-08-19 Adrian Hall Chemical compounds
JP4143413B2 (ja) 2001-03-22 2008-09-03 グラクソ グループ リミテッド β2−アドレナリン受容体アゴニストとしてのホルムアニリド誘導体
WO2002088167A1 (en) 2001-04-30 2002-11-07 Glaxo Group Limited Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha
EP1258247A1 (en) 2001-05-14 2002-11-20 Aventis Pharma Deutschland GmbH Adenosine analogues for the treatment of insulin resistance syndrome and diabetes
EP1395604B1 (en) 2001-06-12 2008-06-25 Glaxo Group Limited Novel anti inflammatory 17.alpha.-heterocyclic-esters of 17.beta.-carbothioate androstane derivatives
EP2327766B1 (en) 2001-06-21 2015-12-02 BASF Enzymes LLC Nitrilases
PL393155A1 (pl) 2001-09-14 2011-03-28 Glaxo Group Limited Pochodne fenetanoloaminy do leczenia chorób układu oddechowego
AU2002362443B2 (en) 2001-10-01 2008-05-15 University Of Virginia Patent Foundation 2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
RU2004110717A (ru) 2001-10-17 2005-10-20 Юсиби, С.А. (Be) Производные хинуклидина, способы их получения и их применение в качестве и нгибиторов м2- и/или м3- мускариновых рецепторов
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
AR037517A1 (es) 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
WO2003048181A1 (en) 2001-12-01 2003-06-12 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
EP1461336B1 (en) 2001-12-20 2013-05-22 CHIESI FARMACEUTICI S.p.A. 1-alkyl-1-azoniabicyclo (2.2.2) octane carbamate derivatives and their use as muscarinic receptor antagonists
WO2003072592A1 (en) 2002-01-15 2003-09-04 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
AU2003201693A1 (en) 2002-01-21 2003-09-02 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
US7414036B2 (en) 2002-01-25 2008-08-19 Muscagen Limited Compounds useful as A3 adenosine receptor agonists
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
JP2005521717A (ja) 2002-03-26 2005-07-21 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用
KR101022977B1 (ko) 2002-03-26 2011-03-18 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도
JP2006515829A (ja) 2002-04-10 2006-06-08 ユニバーシティ オブ バージニア パテント ファウンデーション 炎症性疾病の処置のための、a2aアデノシン受容体アゴニストの使用
US7282591B2 (en) 2002-04-11 2007-10-16 Merck & Co., Inc. 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
JP2005523920A (ja) 2002-04-25 2005-08-11 グラクソ グループ リミテッド フェネタノールアミン誘導体
AU2003239880A1 (en) 2002-05-28 2003-12-12 Theravance, Inc. ALKOXY ARYL Beta2 ADRENERGIC RECEPTOR AGONISTS
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
EP1517895B1 (en) 2002-06-25 2007-03-14 Merck Frosst Canada Ltd. 8-(biaryl) quinoline pde4 inhibitors
AU2003281219A1 (en) 2002-07-02 2004-01-23 Bernard Cote Di-aryl-substituted-ethane pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
EP1521733B1 (en) 2002-07-08 2014-08-20 Pfizer Products Inc. Modulators of the glucocorticoid receptor
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
PE20050130A1 (es) 2002-08-09 2005-03-29 Novartis Ag Compuestos organicos
WO2004018451A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
EP1556049A1 (en) 2002-08-10 2005-07-27 ALTANA Pharma AG Piperidine-pyridazones and phthalazones as pde4 inhibitors
AU2003255376A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
WO2004018450A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-n-oxide-derivatives
AU2003253408A1 (en) 2002-08-17 2004-03-11 Nycomed Gmbh Novel phenanthridines
US20060113968A1 (en) 2002-08-17 2006-06-01 Altana Pharma Ag Novel benzonaphthyridines
AU2003259747A1 (en) 2002-08-21 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
US7288562B2 (en) 2002-08-23 2007-10-30 Ranbaxy Laboratories Limited Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo (3.1.0) hexane derivatives as muscarinic receptor antagonists
JP4587294B2 (ja) 2002-08-29 2010-11-24 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング Pde4インヒビターとしての2−ヒドロキシ−6−フェニルフェナントリジン
AU2003273805B8 (en) 2002-08-29 2010-06-17 Takeda Gmbh 3-hydroxy-6-phenylphenanthridines as PDE-4 inhibitors
CN1678306A (zh) 2002-08-29 2005-10-05 贝林格尔·英格海姆药物公司 在炎性、变应性和增生性疾病中用作糖皮质激素模拟物的3-(磺酰氨基乙基)-吲哚衍生物
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤
KR20050057408A (ko) 2002-09-18 2005-06-16 오노 야꾸힝 고교 가부시키가이샤 트리아자스피로[5.5]운데칸 유도체 및 이를 유효 성분으로하는 약제
CA2499150A1 (en) 2002-09-20 2004-04-01 Merck & Co., Inc. Octahydro-2-h-naphtho[1,2-f] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
AP2005003283A0 (en) 2002-10-11 2005-06-30 Pfizer Indole derivatives useful for the treatment os diseases
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
EP1554264B1 (en) 2002-10-22 2007-08-08 Glaxo Group Limited Medicinal arylethanolamine compounds
AU2003269317B2 (en) 2002-10-23 2009-10-29 Glenmark Pharmaceuticals Ltd. Novel tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
BR0315720A (pt) 2002-10-28 2005-09-06 Glaxo Group Ltd Composto, método para a profilaxia ou tratamento de uma condição clìnica em um mamìmefero, formulação farmacêutica, combinação, uso de um composto, processo para a preparação de um composto, e, intermediário
GB0225287D0 (en) 2002-10-30 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
EP1587818A4 (en) 2003-01-21 2010-10-13 Merck Sharp & Dohme 17-CARBOMOYLOXYCORTISOL DERIVATIVES AS SELECTIVE MODULATORS OF THE GLUCOCORTICOID RECEPTOR
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
EP1460064A1 (en) 2003-03-14 2004-09-22 Pfizer Limited Indole-2-carboxamide derivatives useful as beta-2 agonists
EP1615881A2 (en) 2003-04-01 2006-01-18 Theravance, Inc. Diarylmethyl and related compounds having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
ATE421322T1 (de) 2003-04-04 2009-02-15 Novartis Pharma Gmbh Chinolin-2-on-derivate zur behandlung von erkankungen der atemwege
US7268147B2 (en) 2003-05-15 2007-09-11 Pfizer Inc Compounds useful for the treatment of diseases
ES2329133T3 (es) 2003-05-28 2009-11-23 Theravance, Inc. Compuestos azabicicloalcanicos como antagonistas de receptores de muscarinicos.
WO2004108675A1 (en) 2003-06-04 2004-12-16 Pfizer Limited 2-amino-pyridine derivatives as beta-2 adrenoreceptor agonists
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
DE10332239B3 (de) 2003-07-16 2005-03-03 Framatome Anp Gmbh Zirkoniumlegierung und Bauteile für den Kern von leichtwassergekühlten Kernreaktoren
WO2005033121A2 (en) 2003-10-03 2005-04-14 King Pharmaceuticals Research & Development, Inc. Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs
GB0323701D0 (en) 2003-10-09 2003-11-12 Glaxo Group Ltd Formulations
GB0324654D0 (en) 2003-10-22 2003-11-26 Glaxo Group Ltd Medicinal compounds
GB0324886D0 (en) 2003-10-24 2003-11-26 Glaxo Group Ltd Medicinal compounds
GB0329182D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Chemical compounds
US8025794B2 (en) 2003-12-19 2011-09-27 Shell Oil Company Systems, methods, and catalysts for producing a crude product
DK1699459T3 (da) 2003-12-29 2007-10-08 Can Fite Biopharma Ltd Fremgangsmåde til behandling af multipel sclerose
DE102004001413A1 (de) 2004-01-09 2005-08-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg 3-Hydroxymethyl-4-Hydroxy-Phenyl-Derivate zur Behandlung von chronisch obstruktiver Lungenerkrankung
ATE375977T1 (de) 2004-01-22 2007-11-15 Pfizer Sulfonamidderivate zur behandlung von krankheiten
WO2005080324A1 (en) 2004-01-22 2005-09-01 Pfizer Limited Sulfonamide derivatives for the treatment of diseases
US7320990B2 (en) 2004-02-13 2008-01-22 Theravance, Inc. Crystalline form of a biphenyl compound
DE502005010170D1 (de) 2004-02-14 2010-10-14 Boehringer Ingelheim Pharma Neue langwirksame beta-2-agonisten, und deren verwendung als arzneimittel
JP2007526291A (ja) 2004-03-05 2007-09-13 ケンブリッジ・バイオテクノロジー・リミテッド アデノシン受容体アゴニスト
EP1746885A4 (en) 2004-05-03 2010-09-08 Univ Virginia AGONISTS OF A2A ADENOSINE RECEPTORS FOR THE TREATMENT OF NEEDLE INJURY IN DIABETES
AR049384A1 (es) 2004-05-24 2006-07-26 Glaxo Group Ltd Derivados de purina
US7825102B2 (en) 2004-07-28 2010-11-02 Can-Fite Biopharma Ltd. Treatment of dry eye conditions
WO2006011130A1 (en) 2004-07-28 2006-02-02 Can-Fite Biopharma Ltd. Adenosine a3 receptor agonists for the treatment of dry eye disorders including sjogren’s syndrome
KR20070050484A (ko) 2004-09-09 2007-05-15 더 가브먼트 오브 더 유나이티드 스테이츠 오브 아메리카, 리프리젠티드 바이 더 세크러테리, 디파트먼트 오브 헬쓰 앤드 휴먼 서비씨즈 A1 및 a3 아데노신 수용체 아고니스트로서의 퓨린 유도체
GT200500281A (es) 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
US20080051364A1 (en) 2004-11-08 2008-02-28 Pninna Fishman Therapeutic Treatment of Accelerated Bone Resorption
GB0500785D0 (en) 2005-01-14 2005-02-23 Novartis Ag Organic compounds
SI1848718T1 (sl) * 2005-02-04 2012-12-31 Millennium Pharmaceuticals, Inc. Inhibitorji E1 aktivacijskih enzimov
GB0505219D0 (en) 2005-03-14 2005-04-20 Novartis Ag Organic compounds
GB0514809D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
EP1959939B1 (en) 2005-11-30 2012-01-11 Can-Fite Biopharma Ltd. Use of a3 adenosine receptor agonist in osteoarthritis treatment
DK1983990T3 (da) 2006-01-26 2011-07-11 Us Gov Health & Human Serv Allosteriske A3-adenosin-receptormodulatorer
SI1989206T1 (sl) * 2006-02-02 2012-11-30 Millennium Pharm Inc Inhibitorji e aktivirajočih enzimov
US20080027022A1 (en) 2006-02-08 2008-01-31 Linden Joel M Method to treat gastric lesions
GB0607944D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607945D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
RU2457209C2 (ru) 2006-04-21 2012-07-27 Новартис Аг Производные пурина, предназначенные для применения в качестве агонистов аденозинового рецептора а2а
GB0607951D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607954D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607953D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
EP1889846A1 (en) 2006-07-13 2008-02-20 Novartis AG Purine derivatives as A2a agonists
US8008307B2 (en) * 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
KR20090087054A (ko) 2006-11-10 2009-08-14 노파르티스 아게 시클로펜텐 디올 모노아세테이트 유도체
US20080312160A1 (en) 2007-04-09 2008-12-18 Guerrant Richard L Method of treating enteritis, intestinal damage, and diarrhea from c. difficile with an a2a adenosine receptor agonist
US20080262001A1 (en) 2007-04-23 2008-10-23 Adenosine Therapeutics, Llc Agonists of a2a adenosine receptors for treating recurrent tumor growth in the liver following resection
WO2009006046A1 (en) 2007-06-29 2009-01-08 Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services Dendrimer conjugates of agonists and antagonists of the gpcr superfamily
US20090181934A1 (en) * 2007-10-17 2009-07-16 Novartis Ag Organic Compounds
JP2011500631A (ja) 2007-10-17 2011-01-06 ノバルティス アーゲー アデノシンa1受容体リガンドとしてのプリン誘導体
WO2009061516A1 (en) 2007-11-08 2009-05-14 New York University School Of Medicine Medical implants containing adenosine receptor agonists and methods for inhibiting medical implant loosening
JP2011509305A (ja) 2008-01-09 2011-03-24 ピージーエックスヘルス、リミテッド、ライアビリティー、カンパニー A2arアゴニストによる神経障害性疼痛の髄腔内治療

Also Published As

Publication number Publication date
GT200500281A (es) 2006-04-24
JP2008517027A (ja) 2008-05-22
EP1805181B1 (en) 2012-08-29
ES2394453T3 (es) 2013-01-31
NO20072122L (no) 2007-07-20
US20080200483A1 (en) 2008-08-21
AU2005298878B2 (en) 2009-07-30
AU2009233613A1 (en) 2009-11-26
ECSP077404A (es) 2007-05-30
MA28931B1 (fr) 2007-10-01
JP4904279B2 (ja) 2012-03-28
RU2007118729A (ru) 2008-11-27
CA2582434A1 (en) 2006-05-04
BRPI0517455A (pt) 2008-10-07
US8163754B2 (en) 2012-04-24
MX2007004735A (es) 2007-06-18
WO2006045552A1 (en) 2006-05-04
PE20100266A1 (es) 2010-04-21
NZ554546A (en) 2010-10-29
KR20070073798A (ko) 2007-07-10
AR051642A1 (es) 2007-01-31
EP2292619A1 (en) 2011-03-09
EP1805181A1 (en) 2007-07-11
AU2005298878A1 (en) 2006-05-04
TNSN07154A1 (en) 2008-11-21
RU2403253C2 (ru) 2010-11-10
TW200630366A (en) 2006-09-01
IL182528A0 (en) 2007-09-20

Similar Documents

Publication Publication Date Title
PE20061129A1 (es) Derivados de purina como agonistas del receptor de adenosina a2a
PE20071228A1 (es) Compuestos derivados de purina como activadores del receptor de adenosina a2a
PE20080361A1 (es) Compuestos derivados de purina como activadores del receptor de adenosina a2a
CN1152042C (zh) 部分或完全a1激动剂-n6杂环5’硫代腺苷衍生物
ES2481408T3 (es) Derivados sustituidos de indolilalquilaminas como inhibidores de histona-desacetilasas
ES2587864T3 (es) Derivados de pirimidina
PE20080695A1 (es) Derivados de dihidropirazolopirimidinona como inhibidores de quinasa weel
PE20080944A1 (es) Derivados de pirimidina como inhibidores del receptor de cinasa activina(alk-5)
DK2314594T3 (da) 6-modificerede bicykliske nukleinsyreanaloger
BRPI0606870A2 (pt) composto de indol e uso do mesmo
PE20080951A1 (es) DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS
PE20000270A1 (es) Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol
DK2114925T3 (da) Azetidin-analoger af nucleosidase- og phosphorylase-inhibitorer
PE20110598A1 (es) Inhibidores de las enzimas de proteina cinasa activadas por mitogeno p38
PE20070585A1 (es) Derivados de sulfonamida como activadores de glucoquinasa
PE20110061A1 (es) Derivados de diamino-piridina, pirimidina y piridazina como moduladores del receptor h4 de histamina
PE20071094A1 (es) Derivados 1-ortoflurofenil sustituidos 1,2,5-tiadiazolidindionas como inhibidores de ptpasa
PE20090288A1 (es) Derivados de quinoxalina como inhibidores de la pi3 quinasa
PE20110205A1 (es) Derivados de n-bencensulfonamida-3,4-diamino-3-ciclobuteno-1,2-diona sustituidos como antagonistas del receptor de quimiocina cxcr2
PE20050462A1 (es) COMPUESTOS DE 5,7-DIAMINOPIRAZOLO[4,3-d]PIRIMIDINAS COMO INHIBIDORES DE LA FOSFODIESTERASA TIPO 5 (PDE-5)
PE20081800A1 (es) NUEVOS DERIVADOS DE 3-([1,2,4]TRIAZOLO[4,3-a]PIRIDIN-7-IL)BENZAMIDA
NO20091596L (no) Benzoylamino-heterocykliske forbindelser som Glucokinase-(GLK)-activatorer
EA201001391A1 (ru) Замещенные производные ксантинов и их применение
MX2009010503A (es) Compuestos heterociclicos antiviricos.
CY1113560T1 (el) Αζαϊνδολια χρησιμα ως αναστολεις των jak και αλλων πρωτεϊνικων κινασων

Legal Events

Date Code Title Description
FC Refusal