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DK2614058T3 - Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. - Google Patents

Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. Download PDF

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Publication number
DK2614058T3
DK2614058T3 DK11755311.5T DK11755311T DK2614058T3 DK 2614058 T3 DK2614058 T3 DK 2614058T3 DK 11755311 T DK11755311 T DK 11755311T DK 2614058 T3 DK2614058 T3 DK 2614058T3
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Denmark
Prior art keywords
salt
polymorph
methyl
dimethyl
added
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DK11755311.5T
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English (en)
Inventor
Julie Nicole Hamblin
Paul Spencer Jones
Suzanne Elaine Keeling
Joelle Le
Charlotte Jane Mitchell
Nigel James Parr
Robert David Willacy
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Glaxosmithkline Ip Dev Ltd
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    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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

Claims (14)

1. Polymorf (Form II) af /V-[5-[4-(5-{[(2Æ,6S)-2,6-dimethyl-4-nnorpholinyl]nnethyl}- 1.3- oxazol-2-yl)-l/-/-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, kendet egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved 9,2 ± 0,1.
2. Polymorf ifølge krav 1, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 1 Tabel 1
3. Polymorf ifølge krav 1 eller krav 2 i at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 1.
4. Polymorf (Form III) af /V-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl)·- 1.3- oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, k e n d e t egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved 6,7 ± 0,1.
5. Polymorf ifølge krav 5, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 2 Tabel 2
6. Polymorf ifølge krav 4 eller krav 5, kendetegnet ved, at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 2.
7. Polymorf (Form IV) af /V-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl>- l,3-oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid, kendet egnet ved, at den tilvejebringer et XRPD-mønster omfattende en top (°2Θ) ved omkring 5,8.
8. Polymorf ifølge krav 7, kendetegnet ved, at den tilvejebringer et XRPD-mønster omfattende toppe i alt væsentligt som angivet i tabel 3 Tabel 3
9. Polymorf ifølge krav 7 eller krav 8, kendetegnet ved, at den tilvejebringer et XRPD-mønster i alt væsentligt ifølge figur 3.
10. Salt af /V-[5-[4-(5-{[(2/?,6S)-2,6-dimethyl-4-morpholinyl]methyl>-l,3-oxazol-2-yl)-lH-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid som er natrium-, tosy-lat-, maleat-, hemipamoat-, heminaphthalendisulfonat-, mesitylensulfonat-, hemibiphenyl-disulfonat-, 2-naphthalensulfonat- (napsylat-), hemicinnamat-, hemisebacat-, hemipyro-mellitat- eller hemibenzendiacrylatsaltet.
11. Farmaceutisk sammensætning omfattende en polymorf eller et salt, som defineret i et hvilket som helst af krav 1 til 10 og én eller flere farmaceutisk acceptable excipien-ser.
12. Polymorf eller salt, som defineret i et hvilket som helst af krav 1 til 10 til anvendelse i medicinsk terapi.
13. Polymorf eller salt, som defineret i et hvilket som helst af krav 1 til 10 til anvendelse i behandling af en lidelse medieret af uhensigtsmæssig PI3-kinaseaktivitet.
14. Anvendelse af en polymorf eller et salt, som defineret i et hvilket som helst af krav 1 til 10 til fremstilling af et lægemiddel til anvendelse i behandling af en lidelse medieret af uhensigtsmæssig PI3-kinaseaktivitet.
DK11755311.5T 2010-09-08 2011-09-06 Polymorfer og salte af n-[5-[4-(5-{[(2r,6s)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1h-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methansulfonamid. DK2614058T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38074810P 2010-09-08 2010-09-08
PCT/EP2011/065419 WO2012032067A1 (en) 2010-09-08 2011-09-06 Polymorphs and salts of n- [5- [4- (5- { [(2r,6s) -2, 6 - dimethyl - 4 -morpholinyl] methyl} - 1, 3 - oxazol - 2 - yl) - 1h- inda zol-6-yl] -2- (methyloxy) - 3 - pyridinyl] methanesulfonamide

Publications (1)

Publication Number Publication Date
DK2614058T3 true DK2614058T3 (da) 2015-09-28

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US (1) US8735390B2 (da)
EP (1) EP2614058B1 (da)
JP (1) JP5965402B2 (da)
DK (1) DK2614058T3 (da)
ES (1) ES2548036T3 (da)
HR (1) HRP20151017T1 (da)
HU (1) HUE026059T2 (da)
PL (1) PL2614058T3 (da)
PT (1) PT2614058E (da)
RS (1) RS54286B1 (da)
SI (1) SI2614058T1 (da)
SM (1) SMT201500223B (da)
WO (1) WO2012032067A1 (da)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009147189A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
JP5508400B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド Pi3キナーゼの阻害剤としてのベンズピラゾール誘導体
US8765743B2 (en) 2008-06-05 2014-07-01 Glaxosmithkline Intellectual Property Development Limited Compounds
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
WO2010125082A1 (en) 2009-04-30 2010-11-04 Glaxo Group Limited Oxazole substituted indazoles as pi3-kinase inhibitors
US9102668B2 (en) * 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
WO2012032065A1 (en) * 2010-09-08 2012-03-15 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
WO2012064744A2 (en) * 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
JP6242868B2 (ja) 2012-05-08 2017-12-06 リセラ・コーポレイションLycera Corporation RORγのアゴニストとしての使用のためおよび疾患の処置のためのテトラヒドロ[1,8]ナフチリジンスルホンアミドおよび関連化合物
RU2014149136A (ru) 2012-05-08 2016-07-10 Мерк Шарп И Доум Корп. ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ
NZ702747A (en) 2012-06-13 2017-03-31 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
EA035391B1 (ru) 2012-11-08 2020-06-05 Ризен Фармасьютикалз Са Фармацевтические композиции, содержащие ингибитор pde4 и ингибитор pi3-дельта или двойной ингибитор pi3-дельта-гамма киназы
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
JP6441910B2 (ja) 2013-09-30 2018-12-19 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、中間体、その調製方法、組成物及び使用
CN106831722B (zh) 2013-10-16 2019-08-30 上海璎黎药业有限公司 稠合杂环化合物、其制备方法、药物组合物和用途
RU2016112266A (ru) * 2013-10-17 2017-11-20 Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Ингибитор PI3K для лечения респираторного заболевания
AU2014336250A1 (en) 2013-10-17 2016-04-14 Glaxosmithkline Intellectual Property Development Limited PI3K inhibitor for treatment of respiratory disease
US9663502B2 (en) 2013-12-20 2017-05-30 Lycera Corporation 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease
US9783511B2 (en) 2013-12-20 2017-10-10 Lycera Corporation Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease
US9809561B2 (en) 2013-12-20 2017-11-07 Merck Sharp & Dohme Corp. Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
US10532088B2 (en) 2014-02-27 2020-01-14 Lycera Corporation Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods
EP3209641A4 (en) 2014-05-05 2018-06-06 Lycera Corporation Benzenesulfonamido and related compounds for use as agonists of ror and the treatement of disease
WO2015171610A2 (en) 2014-05-05 2015-11-12 Lycera Corporation Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3256450B1 (en) 2015-02-11 2020-12-02 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
CA2982847A1 (en) 2015-05-05 2016-11-10 Lycera Corporation Dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of ror.gamma. and the treatment of disease
GB201509492D0 (en) * 2015-06-02 2015-07-15 Glaxosmithkline Ip Dev Ltd Novel processes
AU2016276947A1 (en) 2015-06-11 2017-12-14 Lycera Corporation Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORy and the treatment of disease
EP3368535B1 (en) 2015-10-27 2020-12-02 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
AU2016344111A1 (en) 2015-10-27 2018-05-10 Merck Sharp & Dohme Corp. Substituted bicyclic pyrazole compounds as RORgammaT inhibitors and uses thereof
RU2018117503A (ru) 2015-10-27 2019-11-28 Мерк Шарп И Доум Корп. ЗАМЕЩЕННЫЕ ИНДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ RORγТ И ИХ ПРИМЕНЕНИЕ
TWI714820B (zh) * 2017-01-31 2021-01-01 美商基利科學股份有限公司 替諾福韋艾拉酚胺(tenofovir alafenamide)之晶型
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
CZ283425B6 (cs) 1992-04-02 1998-04-15 Smithkline Beecham Corporation Fenylové deriváty a farmaceutické prostředky s jejich obsahem
ES2189322T3 (es) 1994-06-15 2003-07-01 Wellcome Found Intermediarios utiles en la preparacion de inhibidores de encimas.
CA2217950C (en) 1995-04-14 2001-12-25 Glaxo Wellcome Inc. Metered dose inhaler for albuterol
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
TW533865U (en) 1997-06-10 2003-05-21 Glaxo Group Ltd Dispenser for dispensing medicament and actuation indicating device
WO1999016766A1 (en) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Benzodioxole derivatives
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
PT1070056E (pt) 1998-03-14 2004-11-30 Altana Pharma Ag Inibidores de pde iii/iv a base de ftalazinona
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6315112B1 (en) 1998-12-18 2001-11-13 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. Method and package for storing a pressurized container containing a drug
US6352152B1 (en) 1998-12-18 2002-03-05 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
HK1043788A1 (zh) 1999-05-04 2002-09-27 American Home Products Corporation 四環黃體酮受體調節劑化合物及方法
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
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
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
WO2002012265A1 (en) 2000-08-05 2002-02-14 Glaxo Group Limited 6.ALPHA., 9.ALPHA.-DIFLUORO-17.ALPHA.-`(2-FURANYLCARBOXYL) OXY!-11.BETA.-HYDROXY-16.ALPHA.-METHYL-3-OXO-ANDROST-1,4,-DIENE-17-CARBOTHIOIC ACID S-FLUOROMETHYL ESTER AS AN ANTI-INFLAMMATORY AGENT
ES2527688T3 (es) 2000-09-29 2015-01-28 Glaxo Group Limited Derivados de morfolin-acetamida para el tratamiento de enfermedades inflamatorias
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
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
ES2296923T3 (es) 2001-03-22 2008-05-01 Glaxo Group Limited Derivados formanilidas como agonistas del adrenorreceptor beta2.
US7291608B2 (en) 2001-04-30 2007-11-06 Glaxo Group Limited Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α
JP2005500290A (ja) 2001-06-12 2005-01-06 グラクソ グループ リミテッド 抗炎症性の、17β−カルボチオアートアンドロスタン誘導体である17α複素環エステル
ATE417606T1 (de) 2001-09-14 2009-01-15 Glaxo Group Ltd Phenethanolamin-derivate zur behandlung von erkrankungen der atemwege
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
CA2472746A1 (en) 2002-01-14 2003-07-24 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof
US6831093B2 (en) 2002-01-22 2004-12-14 The Regents Of The University Of California Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
PL373043A1 (en) 2002-03-26 2005-08-08 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
CA2477764A1 (en) 2002-03-26 2003-10-09 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
CA2481320A1 (en) 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators
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
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
MXPA05000345A (es) 2002-07-08 2005-03-31 Pfizer Prod Inc Moduladores del receptor de glucocorticoides.
JP2006508042A (ja) 2002-07-18 2006-03-09 ブリストル−マイヤーズ スクイブ カンパニー グルココルチコイド受容体の修飾物質および方法
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
DE60322713D1 (de) 2002-08-21 2008-09-18 Boehringer Ingelheim Pharma Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
NZ538515A (en) 2002-09-16 2007-04-27 Glaxo Group Ltd Pyrazolo[3,4-b]pyridine compounds, and their use as phosphodiesterase inhibitors
EP1542996A4 (en) 2002-09-20 2009-11-18 Merck & Co Inc OCTAHYDRO-2H-NAPHTOc1,2-F INDOL-4-CARBONSUUREAMIDE DERIVATIVES AS SELECTIVE MODULATORS OF THE GLUCOCORTICOID RECEPTOR
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
ES2291733T3 (es) 2002-10-22 2008-03-01 Glaxo Group Limited Compuestos de ariletanolamina medicinales.
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
DK1556342T3 (da) 2002-10-28 2008-07-21 Glaxo Group Ltd Phenethanolaminderivat til behandling af respiratoriske sygdomme
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
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
MXPA06004244A (es) 2003-10-14 2006-06-28 Glaxo Group Ltd Antagonistas del receptor muscarinico de la acetilcolina.
PL1699512T3 (pl) 2003-11-03 2012-11-30 Glaxo Group Ltd Urządzenie do dozowania płynów
AR046225A1 (es) 2003-11-04 2005-11-30 Glaxo Group Ltd Compuesto de 8-azoniabiciclo(3.2.1)octano, composicion farmaceutica para el tratamiento de enfermedades mediadas por receptores de acetilcolina muscarinicos que lo comprende y uso del compuesto para preparar dicha composicion
WO2005058892A1 (en) 2003-12-19 2005-06-30 Glaxo Group Limited Pyrazolo [3,4-b] pyridine compounds, and their use as phosphodiesterase inhibitors
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
AU2005223351A1 (en) 2004-03-16 2005-09-29 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
AR050902A1 (es) 2004-04-27 2006-12-06 Glaxo Group Ltd Compuesto de quinuclidina, composicion farmaceutica que lo comprende y su usopara preparar dicha composicion
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
JP4660553B2 (ja) 2004-10-19 2011-03-30 エフ.ホフマン−ラ ロシュ アーゲー キノリン誘導体
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
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
US8163743B2 (en) * 2008-06-05 2012-04-24 GlaxoGroupLimited 4-carboxamide indazole derivatives useful as inhibitors of PI3-kinases
US8524751B2 (en) * 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
WO2010125082A1 (en) * 2009-04-30 2010-11-04 Glaxo Group Limited Oxazole substituted indazoles as pi3-kinase inhibitors
WO2012032065A1 (en) * 2010-09-08 2012-03-15 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection

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PL2614058T3 (pl) 2015-12-31
HUE026059T2 (en) 2016-05-30
SI2614058T1 (sl) 2015-10-30
EP2614058B1 (en) 2015-07-08
SMT201500223B (it) 2015-10-30
RS54286B1 (sr) 2016-02-29
PT2614058E (pt) 2015-10-27
WO2012032067A1 (en) 2012-03-15
EP2614058A1 (en) 2013-07-17
JP2013537175A (ja) 2013-09-30
JP5965402B2 (ja) 2016-08-03
US20130165441A1 (en) 2013-06-27
ES2548036T3 (es) 2015-10-13
HRP20151017T1 (hr) 2015-10-23

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