EA200970883A1 - Индолкарбоксамиды как ингибиторы ikk2 - Google Patents

Индолкарбоксамиды как ингибиторы ikk2

Info

Publication number
EA200970883A1
EA200970883A1 EA200970883A EA200970883A EA200970883A1 EA 200970883 A1 EA200970883 A1 EA 200970883A1 EA 200970883 A EA200970883 A EA 200970883A EA 200970883 A EA200970883 A EA 200970883A EA 200970883 A1 EA200970883 A1 EA 200970883A1
Authority
EA
Eurasian Patent Office
Prior art keywords
present
relates
ikk2
compound
compounds
Prior art date
Application number
EA200970883A
Other languages
English (en)
Other versions
EA019030B1 (ru
Inventor
Джеффри Чарльз Боэм
Якоб Буш-Петерсен
Вэй Фу
Ци Цзинь
Джеффри К. Кернс
Хуэйцзе Ли
Голян Линь
Сичэнь Линь
Кристофер Э. Нейпп
Original Assignee
Смитклайн Бичам Корпорейшн
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 Смитклайн Бичам Корпорейшн filed Critical Смитклайн Бичам Корпорейшн
Publication of EA200970883A1 publication Critical patent/EA200970883A1/ru
Publication of EA019030B1 publication Critical patent/EA019030B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/382Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

Landscapes

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

Abstract

Настоящее изобретение относится к новым индолкарбоксамидным соединениям. В частности, настоящее изобретение относится к соединениям в соответствии с формулой (I)в которой значения R1, R2, R3, R4 и m определены в описании. Соединения по настоящему изобретению представляют собой ингибиторы IKK2 и могут быть применимы для лечения нарушений, ассоциированных с аномальной активностью IKK2 (также известной как IKKβ), таких как ревматоидный артрит, бронхиальная астма, ринит и COPD (хроническое обструктивное заболевание легких). Соответственно, настоящее изобретение также относится к фармацевтическим композициям, содержащим соединение по настоящему изобретению. Настоящее изобретение также относится к способам ингибирования активности IKK2 и лечения ассоциированных с ней нарушений с использованием соединения по настоящему изобретению или фармацевтической композиции, содержащей соединение по настоящему изобретению.
EA200970883A 2007-03-23 2008-03-20 Индолкарбоксамиды как ингибиторы рецептора ikk2 EA019030B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US89655807P 2007-03-23 2007-03-23
PCT/US2008/057583 WO2008118724A1 (en) 2007-03-23 2008-03-20 Indole carboxamides as ikk2 inhibitors

Publications (2)

Publication Number Publication Date
EA200970883A1 true EA200970883A1 (ru) 2010-04-30
EA019030B1 EA019030B1 (ru) 2013-12-30

Family

ID=39788926

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200970883A EA019030B1 (ru) 2007-03-23 2008-03-20 Индолкарбоксамиды как ингибиторы рецептора ikk2

Country Status (15)

Country Link
US (2) US8071584B2 (ru)
EP (1) EP2139322A4 (ru)
JP (1) JP2010522238A (ru)
KR (1) KR20100015797A (ru)
CN (1) CN101677547A (ru)
AR (1) AR065804A1 (ru)
AU (1) AU2008231105B2 (ru)
BR (1) BRPI0809221A2 (ru)
CA (1) CA2681821A1 (ru)
CL (1) CL2008000829A1 (ru)
EA (1) EA019030B1 (ru)
MX (1) MX2009010270A (ru)
PE (1) PE20081889A1 (ru)
TW (1) TW200901970A (ru)
WO (1) WO2008118724A1 (ru)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0400895D0 (en) * 2004-01-15 2004-02-18 Smithkline Beecham Corp Chemical compounds
AR050253A1 (es) * 2004-06-24 2006-10-11 Smithkline Beecham Corp Compuesto derivado de indazol carboxamida, composicion que lo comprende y su uso para la preparacion de un medicamento
US8063071B2 (en) 2007-10-31 2011-11-22 GlaxoSmithKline, LLC Chemical compounds
JP2009516702A (ja) * 2005-11-18 2009-04-23 スミスクライン・ビーチャム・コーポレイション 化合物
EP2064175B1 (en) 2006-09-07 2014-08-06 F. Hoffmann-La Roche AG A process for the manufacture of snac (salcaprozate sodium)
PE20081889A1 (es) 2007-03-23 2009-03-05 Smithkline Beecham Corp Indol carboxamidas como inhibidores de ikk2
US8354539B2 (en) 2009-03-10 2013-01-15 Glaxo Group Limited Indole derivatives as IKK2 inhibitors
ES2627085T3 (es) 2010-05-07 2017-07-26 Glaxosmithkline Llc Indoles
ES2708998T3 (es) * 2013-06-26 2019-04-12 Abbvie Inc Carboxamidas primarias como inhibidores de btk
US9975844B2 (en) 2014-04-17 2018-05-22 Sumitomo Chemical Company, Limited Method for producing nitro compound
US20160168089A1 (en) * 2014-12-12 2016-06-16 H. Lundbeck A/S Process for the manufacture of idalopirdine
MA41148A (fr) * 2014-12-12 2017-10-17 H Lundbeck As Procédé de fabrication d'idalopirdine
CA3060715A1 (en) * 2017-04-24 2018-11-01 Tesaro, Inc. Methods of manufacturing of niraparib
CN113024506B (zh) * 2021-03-18 2022-05-20 合肥工业大学 3-甲酰四氢噻喃化合物的制备方法

Family Cites Families (192)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2064336B (en) 1979-12-06 1984-03-14 Glaxo Group Ltd Device for dispensing medicaments
US4353656A (en) 1980-10-14 1982-10-12 Xerox Corporation Moving coil, multiple energy print hammer system including a closed loop servo
DE3274065D1 (de) 1981-07-08 1986-12-11 Draco Ab Powder inhalator
US4778054A (en) 1982-10-08 1988-10-18 Glaxo Group Limited Pack for administering medicaments to patients
GB2169265B (en) 1982-10-08 1987-08-12 Glaxo Group Ltd Pack for medicament
GR79615B (ru) 1982-10-08 1984-10-31 Glaxo Group Ltd
US4775761A (en) * 1983-08-22 1988-10-04 Hoechst-Roussel Pharmaceuticals, Inc. 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles
DE3342632A1 (de) 1983-11-25 1985-06-05 Merck Patent Gmbh, 6100 Darmstadt Indolderivate
US5256673A (en) 1983-11-25 1993-10-26 Merck Patent Gesellschaft Mit Beschrankter Haftung Indole-3-yl-A-tetrahydropyridyl or piperidyl compounds
US4811731A (en) 1985-07-30 1989-03-14 Glaxo Group Limited Devices for administering medicaments to patients
DE3882732T2 (de) 1987-02-10 1993-12-02 Abbott Lab Indol, Benzofuran, Benzothiophen enthaltende, Lipoxygenase hemmende Verbindungen.
JPH0262875A (ja) * 1988-05-23 1990-03-02 Wakunaga Pharmaceut Co Ltd 新規イソインドリン誘導体
PH30133A (en) 1989-09-07 1997-01-21 Abbott Lab Indole-, benzofuran-, and benzothiophene-containing lipoxygenase inhibiting compounds
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
US5254473A (en) 1990-03-16 1993-10-19 Jp Laboratories Solid state device for monitoring integral values of time and temperature of storage of perishables
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
JP2963288B2 (ja) 1992-01-14 1999-10-18 株式会社海洋バイオテクノロジー研究所 水中有害付着生物防除剤
AU677776B2 (en) 1992-04-02 1997-05-08 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
US5256873A (en) * 1992-09-03 1993-10-26 Eaton Corporation Multiple station through beam photoelectric sensor
US5330986A (en) 1992-11-24 1994-07-19 Hoechst-Roussel Pharmaceuticals Inc. Indole-7-carboxamide derivatives
FR2701026B1 (fr) 1993-02-02 1995-03-31 Adir Nouveaux dérivés de l'indole, de l'indazole et du benzisoxazole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
WO1994021627A1 (en) 1993-03-18 1994-09-29 Merck Sharp & Dohme Limited Indole derivatives as dopamine d4 antagonists
GB9305623D0 (en) 1993-03-18 1993-05-05 Merck Sharp & Dohme Therapeutic agents
CN1048015C (zh) * 1993-07-06 2000-01-05 美国辉瑞有限公司 双环四氢吡唑并吡啶类化合物
CN1070849C (zh) 1994-06-15 2001-09-12 惠尔康基金会集团公司 酶抑制剂
ZA951822B (en) 1994-12-23 1996-09-26 Glaxo Group Ltd Chemical compounds
DE19500689A1 (de) 1995-01-12 1996-07-18 Merck Patent Gmbh Indolpiperidin-Derivate
CA2213442A1 (en) 1995-03-10 1996-09-19 The Minnesota Mining & Manufacturing Company Aerosol valves
CN1192680A (zh) 1995-06-07 1998-09-09 苏根公司 抑制接合蛋白/酪氨酸激酶相互作用的方法与组合物
GB9610811D0 (en) 1996-05-23 1996-07-31 Pharmacia Spa Combinatorial solid phase synthesis of a library of indole derivatives
EP1077213A3 (en) 1996-06-14 2001-06-13 Eli Lilly And Company Inhibition of serotonin reuptake
US5846982A (en) 1996-06-14 1998-12-08 Eli Lilly And Company Inhibition of serotonin reuptake
JP2001506230A (ja) 1996-08-09 2001-05-15 スミスクライン・ビーチャム・コーポレイション 新規ピペラジン含有化合物
WO1998028292A1 (en) 1996-12-23 1998-07-02 Smithkline Beecham Corporation Novel piperidine containing compounds
GB9700226D0 (en) 1997-01-08 1997-02-26 Glaxo Group Ltd Inhalation device
MY117948A (en) 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
HUP0002929A3 (en) 1997-08-06 2002-01-28 Lilly Co Eli 2-acylaminopropanamines as tachykinin receptor antagonists and pharmaceutical compositions containing the same
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
AR013669A1 (es) 1997-10-07 2001-01-10 Smithkline Beecham Corp Compuestos y metodos
DE19756036A1 (de) 1997-12-17 1999-06-24 Merck Patent Gmbh Amid- und Harnstoffderivate
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
DE19807993A1 (de) 1998-02-26 1999-09-02 Bayer Ag Verwendung von ß-Carbolinderivaten zur Bekämpfung von TNF-alpha-abhängigen Krankheiten
BR9908301A (pt) 1998-02-27 2000-10-31 Kissei Pharmaceutical Derivados de indol e composições farmacêuticas que compreendem os mesmos
SI1070056T1 (en) 1998-03-14 2004-12-31 Altana Pharma Ag Phthalazinone pde iii/iv inhibitors
US6589954B1 (en) * 1998-05-22 2003-07-08 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
JP2002519348A (ja) 1998-06-30 2002-07-02 イーライ・リリー・アンド・カンパニー 5−ht1fアゴニスト
RS50340B (sr) 1999-06-23 2009-11-10 Sanofi-Aventis Deutschland Gmbh., Supstituisani benzimidazoli
DE19928424A1 (de) 1999-06-23 2000-12-28 Aventis Pharma Gmbh Substituierte Benzimidazole
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
CA2380373A1 (en) * 1999-08-13 2001-02-22 Seth Lederman Cyclobenzaprine for treating generalized anxiety disorder and compositions thereof
CO5180649A1 (es) 1999-09-01 2002-07-30 Abbott Lab Antagonistas de los receptores de los glucocorticoides para el tratamiento de la diabetes para el tratamiento de la diabetes
DE19951360A1 (de) 1999-10-26 2001-05-03 Aventis Pharma Gmbh Substituierte Indole
US6245799B1 (en) * 1999-11-08 2001-06-12 American Home Products Corp [(Indol-3-yl)-cycloalkyl]-3-substituted azetidines for the treatment of central nervous system disorders
JP2003513970A (ja) 1999-11-08 2003-04-15 ワイス 中枢神経系障害の治療のための[(インドール−3−イル)−シクロアルキル]−3−置換アゼチジン
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
US6632666B2 (en) 2000-01-14 2003-10-14 Biolife Solutions, Inc. Normothermic, hypothermic and cryopreservation maintenance and storage of cells, tissues and organs in gel-based media
GB0003154D0 (en) 2000-02-12 2000-04-05 Astrazeneca Uk Ltd Novel compounds
WO2001068648A1 (en) 2000-03-15 2001-09-20 Aventis Pharma Deutschland Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity
EP1209158A1 (en) 2000-11-18 2002-05-29 Aventis Pharma Deutschland GmbH Substituted beta-carbolines
EP1134221A1 (en) 2000-03-15 2001-09-19 Aventis Pharma Deutschland GmbH Substituted beta-carbolines as lkB kinase inhibitors
AU5553801A (en) * 2000-04-24 2001-11-07 Bristol Myers Squibb Co Heterocycles that are inhibitors of impdh enzyme
BR0110420A (pt) 2000-04-28 2003-07-01 Acadia Pharm Inc Agonistas muscarìnicos
WO2001087298A1 (fr) 2000-05-15 2001-11-22 Rohto Pharmaceutical Co., Ltd. Preparation liquide a base d'eau
US6414013B1 (en) 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
US20050009876A1 (en) 2000-07-31 2005-01-13 Bhagwat Shripad S. Indazole compounds, compositions thereof and methods of treatment therewith
US6897231B2 (en) 2000-07-31 2005-05-24 Signal Pharmaceuticals, Inc. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
OA12394A (en) 2000-08-05 2004-07-09 Glaxo Group Ltd 6.Alpha-,9.alpha.-difluoro-17.alpha.-'(2-furanylcarboxyl)oxyl-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4,-diene-17-carbothioic acid s-fuoromethyl ester as an anti-inflammatory agent.
MXPA03001420A (es) 2000-08-14 2004-01-26 Johnson & Johnson Pirazoles sustituidos.
US20030171413A1 (en) 2000-08-17 2003-09-11 Owen David Alan Bicyclic heteroaromatic derivatives for the treatment of immune and inflammatory disorders
US6868504B1 (en) * 2000-08-31 2005-03-15 Micron Technology, Inc. Interleaved delay line for phase locked and delay locked loops
EP1315741A2 (en) * 2000-09-06 2003-06-04 Ortho-McNeil Pharmaceutical, Inc. A method for treating allergies
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
KR20030031198A (ko) 2000-09-29 2003-04-18 글락소 그룹 리미티드 염증 질환 치료용 모르폴린-아세트아미드 유도체
US6869956B2 (en) 2000-10-03 2005-03-22 Bristol-Myers Squibb Company Methods of treating inflammatory and immune diseases using inhibitors of IκB kinase (IKK)
US6960585B2 (en) 2000-10-03 2005-11-01 Bristol-Myers Squibb Company Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
WO2002030423A1 (en) 2000-10-12 2002-04-18 Smithkline Beecham Corporation NF-λB INHIBITORS
WO2002030353A2 (en) 2000-10-12 2002-04-18 Smithkline Beecham Corporation NF-λB INHIBITORS
BR0114978A (pt) 2000-10-26 2004-04-20 Tularik Inc Composições e métodos que são úteis no tratamento de condições ou doenças inflamatórias, metabólicas, e proliferativas celulares
JP2002193938A (ja) 2000-12-01 2002-07-10 Bayer Ag 4−アリールピリジン誘導体
US7122544B2 (en) 2000-12-06 2006-10-17 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
DK1355904T3 (da) 2000-12-22 2007-10-15 Wyeth Corp Heterocyclindazol- og -azaindazolforbindelser som 5-hydroxytryptamin-6-ligander
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
CZ20032287A3 (cs) 2001-02-01 2004-02-18 Bristol-Myers Squibb Company Způsoby léčení zánětlivých a imunitních nemocí za použití inhibitorů IkB kinázy (IKK)
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
US7144908B2 (en) 2001-03-08 2006-12-05 Glaxo Group Limited Agonists of beta-adrenoceptors
DE10112151A1 (de) 2001-03-14 2002-09-19 Merck Patent Gmbh Substituierte Benzofuran-2-carbonsäureamide
US7045658B2 (en) 2001-03-22 2006-05-16 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
EP2039700A2 (en) 2001-04-30 2009-03-25 Glaxo Group Limited Novel anti-inflammatory androstane derivatives
BR0209930A (pt) 2001-05-24 2004-03-30 Leo Pharma As Composto, composição farmacêutica, método para tratar doenças proliferativas, e, uso de um composto
US20030045515A1 (en) 2001-05-24 2003-03-06 Lise Binderup Combination medicament for treatment of neoplastic diseases
WO2002094265A1 (en) 2001-05-24 2002-11-28 Leo Pharma A/S A method of modulating nf-$g(k)b activity
NZ529631A (en) 2001-06-07 2006-08-31 F Indole derivatives with 5-hydroxytryptamine (5-HT) 5-HT6 receptor affinity in the treatment of disorders of the CNS
ATE399174T1 (de) 2001-06-12 2008-07-15 Glaxo Group Ltd Neue anti inflammatorische 17.alpha.- heterozyklische ester von 17.beta.-carbothioat androstan derivativen
US6638679B2 (en) 2001-07-12 2003-10-28 Kodak Polychrome Graphics, Llc Photosensitive compositions having mixtures of alkoxy and non-alkoxy diazonium salt containing compounds
SE0102616D0 (sv) 2001-07-25 2001-07-25 Astrazeneca Ab Novel compounds
SE0102617D0 (sv) 2001-07-25 2001-07-25 Astrazeneca Ab Novel compounds
US20030127204A1 (en) 2001-09-06 2003-07-10 Varnell Daniel F. Amphoteric polymer resins that increase the rate of sizing development
PT1425001E (pt) 2001-09-14 2009-02-18 Glaxo Group Ltd Derivados de fenetanolamina para o tratamento de doenças respiratórias
JP2005506983A (ja) 2001-09-19 2005-03-10 ファルマシア・コーポレーション 炎症の治療のための置換ピラゾリル化合物
BR0212613A (pt) 2001-09-19 2004-08-31 Pharmacia Corp Compostos de indazol substituìdos para o tratamento de inflamação
MXPA04002683A (es) 2001-09-19 2004-06-18 Pharmacia Corp Compuestos bencenosulfamida pirazolil sustituidos para el tratamiento de la inflamacion.
WO2003024936A1 (en) 2001-09-19 2003-03-27 Pharmacia Corporation Substituted pyrazolo compounds for the treatment of inflammation
JP2005509645A (ja) 2001-10-30 2005-04-14 ファルマシア・コーポレーション 炎症処置用のヘテロ芳香族カルボキサミド誘導体
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
DE60309829T2 (de) 2002-01-14 2007-09-13 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Glucocorticoidmimetika, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische formulierungen und ihre verwendungen
JP4745609B2 (ja) 2002-01-22 2011-08-10 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用
US6646785B2 (en) 2002-01-31 2003-11-11 Corning Incorporated Fiber ring amplifiers and lasers
DK1476136T3 (da) 2002-02-14 2006-10-09 Glaxo Group Ltd Farmaceutisk præparat, der omfatter N-[(1-N-butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indol-10-carboxamid eller salt, og fremgangsmåde derfor, der omfatter törgranulering
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
MXPA04009329A (es) 2002-03-26 2005-01-25 Boehringer Ingelheim Pharma Mimeticos de glucocorticoides, metodos para su preparacion, composiciones farmaceuticas y usos de los mismos.
US7268152B2 (en) 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
AU2003222106A1 (en) 2002-04-03 2003-10-20 Bristol-Myers Squibb Company Thiopene-based tricyclic compounds and pharmaceutical compositions comprising same
EP1495016A2 (en) 2002-04-09 2005-01-12 Astex Technology Limited Heterocyclic compounds and their use as modulators of p38 map kinase
DE60335869D1 (de) 2002-04-11 2011-03-10 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
TW200403991A (en) 2002-04-11 2004-03-16 Smithkline Beecham Corp NF-κb inhibitors
US7271197B2 (en) 2002-04-25 2007-09-18 Glaxo Group Limited Phenethanolamine derivatives
WO2003095430A1 (en) 2002-05-09 2003-11-20 Pharmacia Corporation Substituted pyrazolyl compounds for the treatment of inflammation
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE60307102T2 (de) 2002-05-30 2006-12-07 Neurosearch A/S 3-substituierte chinuclidine und ihre verwendung
EP1513516B1 (en) 2002-06-06 2008-12-03 Boehringer Ingelheim Pharmaceuticals Inc. SUBSTITUTED 3-AMINO-THIENO(2,3-b) PYRIDINE-2-CARBOXYLIC ACID AMIDE COMPOUNDS AND PROCESSES FOR PREPARING AND THEIR USES
JP2005531608A (ja) 2002-06-06 2005-10-20 スミスクライン・ビーチャム・コーポレイション NF−κB阻害剤
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2004005229A1 (en) 2002-07-08 2004-01-15 Pfizer Products Inc. Modulators of the glucocorticoid receptor
WO2004009017A2 (en) 2002-07-18 2004-01-29 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
DE10237722A1 (de) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
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
RS20050174A (en) 2002-08-29 2007-06-04 Boehringer Ingelheim Pharmaceuticals Inc., -3(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
US6911445B2 (en) 2002-09-12 2005-06-28 Wyeth Antidepressant cycloalkylamine derivatives of heterocycle-fused benzodioxans
US7135479B2 (en) 2002-09-12 2006-11-14 Wyeth Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
PL375993A1 (en) 2002-09-16 2005-12-12 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compounds, and their use as phosphodiesterase inhibitors
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
JP4520309B2 (ja) 2002-09-20 2010-08-04 メルク・シャープ・エンド・ドーム・コーポレイション 選択的糖質コルチコイド受容体調節剤としてのオクタヒドロ−2−H−ナフト[1,2−f]インドール−4−カルボキサミド誘導体
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
EP1554264B1 (en) 2002-10-22 2007-08-08 Glaxo Group Limited Medicinal arylethanolamine compounds
AU2003286143A1 (en) 2002-10-28 2004-05-13 Glaxo Group Limited Phenethanolamine derivative for the treatment of respiratory diseases
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
JP4401298B2 (ja) 2002-12-02 2010-01-20 エフ.ホフマン−ラ ロシュ アーゲー Crfアンタゴニストとしてのインダゾール誘導体
WO2004053087A2 (en) 2002-12-06 2004-06-24 Smithkline Beecham Corporation Nf-κb inhibitors
DE10259244A1 (de) 2002-12-17 2004-07-01 Merck Patent Gmbh N-(Indolethyl-)cycloamin-Verbindungen
US7329668B2 (en) 2003-02-25 2008-02-12 Bristol-Myers Squibb Company Pyrazolopurine-based tricyclic compounds and pharmaceutical compositions comprising same
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
US7176214B2 (en) 2003-05-21 2007-02-13 Bristol-Myers Squibb Company Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
JP2007533602A (ja) 2003-07-31 2007-11-22 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 置換ベンゾチオフェン化合物及びそれらの使用
US7291733B2 (en) 2003-10-10 2007-11-06 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted tricyclic heterocycles and their uses
DE602004005881T2 (de) 2003-10-14 2008-01-17 Pharmacia Corp. Substituierte pyrazinonverbindungen zur behandlung von entzündungen
EA013689B1 (ru) 2003-10-14 2010-06-30 Глэксо Груп Лимитед Антагонисты мускариновых ацетилхолиновых рецепторов
PE20050489A1 (es) 2003-11-04 2005-09-02 Glaxo Group Ltd Antagonistas de receptores de acetilcolina muscarinicos
EP2065383A1 (en) 2003-11-19 2009-06-03 Signal Pharmaceuticals, Inc. Indazole compounds and methods of use thereof as protein kinase inhibitors
WO2005058892A1 (en) 2003-12-19 2005-06-30 Glaxo Group Limited Pyrazolo [3,4-b] pyridine compounds, and their use as phosphodiesterase inhibitors
JP2007514759A (ja) 2003-12-19 2007-06-07 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
GB0400895D0 (en) * 2004-01-15 2004-02-18 Smithkline Beecham Corp Chemical compounds
DE102004012069A1 (de) 2004-03-12 2005-09-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue aryl-haltige 5-Acylindolinone, deren Herstellung und deren Verwendung als Arzneimittel
EP1735314A1 (en) 2004-03-16 2006-12-27 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
UY28871A1 (es) 2004-04-27 2005-11-30 Glaxo Group Ltd Antagonistas del receptor de acetilcolina muscarinico
AR050253A1 (es) 2004-06-24 2006-10-11 Smithkline Beecham Corp Compuesto derivado de indazol carboxamida, composicion que lo comprende y su uso para la preparacion de un medicamento
WO2006000401A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited Substituted oxazines as glucocorticoid receptor modulators
WO2006000398A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
TW200626142A (en) * 2004-09-21 2006-08-01 Glaxo Group Ltd Chemical compounds
RU2391338C2 (ru) 2004-10-19 2010-06-10 Ф.Хоффманн-Ля Рош Аг Производные хинолина
EP1841780B1 (en) 2005-01-10 2011-07-27 Glaxo Group Limited Androstane 17-alpha-carbonate derivatives for use in the treatment of allergic and inflammatory conditions
US20090124588A1 (en) 2005-01-10 2009-05-14 Glaxo Group Limited Androstane 17-Alpha-Carbonate for Use in the Treatment of Inflammatory and Allergic Conditions
JP2008534664A (ja) 2005-04-06 2008-08-28 アストラゼネカ アクチボラグ 置換複素環およびchk1、pdk1及びpak阻害剤としてのそれらの使用
ZA200709038B (en) 2005-04-13 2009-01-28 Neuraxon Inc Substituted indole compounds having nos inhibitory activity
ES2535136T3 (es) 2005-06-14 2015-05-05 Construction Research & Technology Gmbh Provisión de resistencia a la congelación y descongelación a composiciones cementosas
UA99699C2 (ru) * 2005-06-30 2012-09-25 Смитклайн Бичам Корпорейшн Производные индолкарбоксамида и фармацевтическая композиция, которая их содержит
US8063071B2 (en) * 2007-10-31 2011-11-22 GlaxoSmithKline, LLC Chemical compounds
EP1916245B1 (en) 2005-07-22 2011-10-26 Shionogi & Co., Ltd. Indole derivative having pgd2 receptor antagonist activity
JP2009513677A (ja) 2005-10-25 2009-04-02 スミスクライン・ビーチャム・コーポレイション 化合物
EP1940296A2 (en) 2005-10-25 2008-07-09 SmithKline Beecham Corporation Chemical compounds
JP2009516702A (ja) * 2005-11-18 2009-04-23 スミスクライン・ビーチャム・コーポレイション 化合物
JP2009519968A (ja) * 2005-12-16 2009-05-21 スミスクライン・ビーチャム・コーポレイション 化学物質
JP5255559B2 (ja) 2006-03-31 2013-08-07 アボット・ラボラトリーズ インダゾール化合物
CL2007002708A1 (es) 2006-09-22 2008-04-04 Glaxo Group Ltd Compuestos derivados de pirrolo[2,3-b]piridina; procedimiento de preparacion; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, caquexia, trastornos inflamatorios, entre otros.
PE20081889A1 (es) 2007-03-23 2009-03-05 Smithkline Beecham Corp Indol carboxamidas como inhibidores de ikk2
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
GB0804592D0 (en) 2008-03-12 2008-04-16 Glaxo Group Ltd Novel compounds
US8354539B2 (en) 2009-03-10 2013-01-15 Glaxo Group Limited Indole derivatives as IKK2 inhibitors
JP2012520845A (ja) 2009-03-17 2012-09-10 グラクソ グループ リミテッド Itk阻害剤として使用されるピリミジン誘導体

Also Published As

Publication number Publication date
US20120040958A1 (en) 2012-02-16
PE20081889A1 (es) 2009-03-05
CN101677547A (zh) 2010-03-24
EP2139322A4 (en) 2011-04-06
TW200901970A (en) 2009-01-16
AU2008231105B2 (en) 2011-07-21
CL2008000829A1 (es) 2008-09-26
BRPI0809221A2 (pt) 2019-09-24
KR20100015797A (ko) 2010-02-12
AR065804A1 (es) 2009-07-01
EP2139322A1 (en) 2010-01-06
WO2008118724A1 (en) 2008-10-02
CA2681821A1 (en) 2008-10-02
MX2009010270A (es) 2009-10-12
US8071584B2 (en) 2011-12-06
US8372875B2 (en) 2013-02-12
US20100130468A1 (en) 2010-05-27
AU2008231105A1 (en) 2008-10-02
JP2010522238A (ja) 2010-07-01
EA019030B1 (ru) 2013-12-30

Similar Documents

Publication Publication Date Title
EA200970883A1 (ru) Индолкарбоксамиды как ингибиторы ikk2
TW200616967A (en) Novel indazole carboxamides and their use
MY154895A (en) Pyrimidine hydrazide compounds as pgds inhibitors
MY151172A (en) Pyrimidine amide compounds as pgds inhibitors
ATE530540T1 (de) Pyrimidonverbindungen als gsk-3-inhibitoren
MA32393B1 (fr) Composés et compositions servant d'inhibiteurs de kinases
EA200800183A1 (ru) Новые производные индолкарбоксамида, содержащая их фармацевтическая композиция и способ лечения
WO2007076286A3 (en) Chemical compounds
EA201170520A1 (ru) Ингибитор p38 mapk-киназы
TW200626142A (en) Chemical compounds
MX2009004289A (es) Compuestos triciclicos como inhibidores de metaloproteinasas matriciales.
MX2010001486A (es) Derivados de tetrahidropiridin carboxamida como antagonistas de trpvl.
NO20083918L (no) Dihydridiazepiner anvendelige som inhibitorer av proteinkinaser
EA200900983A1 (ru) Соединения и композиции в качестве ингибиторов киназы
EA200970337A1 (ru) Ингибиторы котранспортера натрий-глюкозы 2 и способы их применения
MX2009010960A (es) Compuestos heterociclicos y sus metodos de uso.
WO2007102883A3 (en) Chemical compounds
UA92636C2 (en) Tetrahydro-pyrimidoazepines as modulators of trpv1
MX350862B (es) Acidos de piperidinil naftilacetico.
WO2007062318A3 (en) Chemical compounds
MX2010004498A (es) Derivados de ciclohexenoamida y su uso como antagonistas de trpv1.
WO2006086609A3 (en) Inhibitors of tryptase
NO20092719L (no) Nye kromen-2-on-derivater og deres anvendelse som monoaminneurotransmitter-gjenopptaksinhibitorer
NO20081483L (no) Kombinasjon av forbindelser som kan brukes ved behandling av respiratoriske sykdommer, spesielt kronisk obstruktiv pulmonaer sykdom (COPD) og astma
EA201270265A1 (ru) Ингибиторы катепсина с

Legal Events

Date Code Title Description
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 BY KZ KG MD TJ TM RU