ME02053B - Oksazol supstituisani indazoli kao inhibitori pi3-kinaze - Google Patents

Oksazol supstituisani indazoli kao inhibitori pi3-kinaze

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Publication number
ME02053B
ME02053B MEP-2015-22A MEP2215A ME02053B ME 02053 B ME02053 B ME 02053B ME P2215 A MEP2215 A ME P2215A ME 02053 B ME02053 B ME 02053B
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ME
Montenegro
Prior art keywords
oxazol
salt
methyl
compound
compound according
Prior art date
Application number
MEP-2015-22A
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English (en)
Inventor
David A Mareska
Julie Nicole Hamblin
Suzanne Elaine Keeling
Joelle Le
Charlotte Jane Mitchell
Nigel James Parr
Original Assignee
Glaxo Group Ltd
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Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of ME02053B publication Critical patent/ME02053B/me

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Claims (23)

1.Jedinjenje formule (I):gdeR1 je 9- ili 10-člani biciklični heteroaril, pri čemu 9- ili 10-člani biciklični heteroaril sadrži od jedan do tri heteroatoma nezavisno izabrana od kiseonika i azota i opciono supstituisan sa C1-6alkil, C3-6cikloalkil, halo, -CN ili - NHSO2R5, ilipiridinil opciono supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-6alkil, -OR6, halo i –NHSO2R7;R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6- ili 7-člani heterocikl pri čemu 6- ili 7-člani heterocikl opciono sadrži atom kiseonika ili drugi atom azota i opciono je supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-6alkil;R4 je vodonik ili metil;R6 je vodonik C1-4alkil; iR5 i R7 su svaka nezavisno C1-6alkil, ili fenil opciono supstituisan sa jednim ili dva supstituenta nezavisno izabrana od halo;ili njegova so.
2.Jedinjenje prema zahtevu 1, ili njegova so, gde R1 je 9-člani biciklični heteroaril pri čemu 9-člani biciklični heteroatom sadrži jedan ili dva atoma azota, ili piridinil opciono supstituisan sa jednim ili dva supstituenta izabrana od -OR6 i-NHSO2R7.
3.Jedinjenje prema zahtevu 1 ili zahtevu 2, ili njegova so, gde je R1 indolil.
4.Jedinjenje prema zahtevu 1 ili zahtevu 2, ili njegova so, gde je R1 piridinil opciono supstituisan sa jednim ili dva supstituenta nazavisno izabrana od - OR6 i -NHSO2R7.
5.Jedinjenje prema bilo kom od prethodnih zahteva, ili njegova so, gde R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6-člani heterocikl pri čemu 6-člani heterocikl opciono sadrži atom kiseonika ili drugi atom azota i opciono je supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-6 alkila.
6.Jedinjenje prema bilo kom od prethodnih zahteva, ili njegova so, gde R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6-člani heterocikl pri čemu 6-člani heterocikl sadrži atom kiseonika i opciono je supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-4 alkila.
7.Jedinjenje prema bilo kom od zahteva 1 do 5, ili njegova so, gde R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6-člani heterocikl u kome 6-člani heterocikl sadrži drugi atom azota i opciono je supstituisan sa C1-4 alkil.
8.Jedinjenje prema bilo kom od prethodnih zahteva, ili njegova so, gde je R4 vodonik.
9.Jedinjenje prema zahtevu 1, koje je: N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid; N-[5-[4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid; N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]-2,4-difluorobenzensulfonamid; 2,4-difluoro-N-[5-[4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]benzensulfonamid; 4-((5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-6-(1H-indol-4-il)-1H-indazol; 6-((1H-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol; 6-((1H-indol-4-il)-4-[5-(4-morfolinilmetil)-1,3-oksazol-2-il]-1H-indazol; N-[5-[4-(5-{[(2R,6R)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid; 6-((1H-indol-4-il)-4-[5-(1-piperazinilmetil)-1,3-oksazol-2-il]-1H-indazol; ili njegova so.
10.Jedinjenje prema zahtevu 1, koje je: N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid ili njegova so.
11.Jedinjenje prema zahtevu 1 koje je: 6-((1H-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol ili njegova so.
12.Jedinjenje prema bilo kom od zahteva 1 do 11 u obliku njegove farmaceutski prihvatljive soli.
13.Jedinjenje prema zahtevu 11 u obliku soli sukcinata.
14.Jedinjenje prema zahtevu 1, koje je: N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid
15.Jedinjenje prema zahtevu 1 koje je: 6-((1H-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol
16.Farmaceutska kompozicija sadrži jedinjenje koje je definisano u bilo kom od patentnih zahteva 1 do 11, ili njegova farmaceutski prihvatljiva so, i jedan ili više farmaceutski prihvatljivih ekscipijenata.
17.Jedinjenje definisano prema bilo kom od zatheva 1 do 11, ili njegova farmaceutski prihvatljiva so, za upotrebu u medicinskoj terapiji.
18.Jedinjenje definisano prema bilo kom od zahteva 1 do 11, ili njegova farmaceutski prihvatljiva so, za upotrebu u lečenju poremećaja posredovanog neodgovarajućom aktivnošću PI-3-kinaze.
19.Upotreba jedinjenja kako je definisano prema bilo kom od patentnih zahteva 1 do 11, ili njegova farmaceutski prihvatljiva so u proizvodnji leka za upotrebu u lečenju poremećaja posredovanog neodgovarajućom aktivnošću PI3-kinaze.
20.Jedinjenje za upotrebu prema zahtevu 18, gde poremećaj posredovan neodgovarajućom aktivnošću PI3-kinaze je respiratorna bolest, virusna infekcija, nevirusna respiratorna infekcija, alergijska bolest, autoimuna bolest, inflamatorna bolest, kardiovaskularna bolest, hematološki malignitet, neurodegenerativna bolest, pankreatitis, višestruko otkazivanje organa, bolest bubrega, agregacija krvnih pločica, kancer, pokretljivost sperme, odbacivanje transplanta, odbacivanje grafta, povreda pluća ili bol.
21.Jedinjenje za upotrebu prema zahtevu 18, gde je poremećaj posredovan neodgovarajućom aktivnošću PI3-kinaze astma, hronična obstruktivna bolest pluća (COPD), idiopatska pulmonarna fibroza (IPF), virusne infekcije respiratornog trakta, virusno pogoršanje respiratornih bolesti, aspergiloza, lajšmanijaza, alergijski rinitis, atopični dermatitis, reumatoidni artritis, multipla skleroza, inflamatorna bolest creva, tromboza, ateroskleroza, hematološki malignitet, neurodegenerativna bolest, pankreatitis, višestruko otkazivanje organa, bolest bubrega, agregacija krvnih pločica, kancer, pokretnljivost sperme, odbacijavanje transplanta, odbacivanje grafta, povreda pluća, bol u vezi sa reumatoidnim artritisom ili oesteoartritisom, bol u leđima, generalni inflamatorni bol, posthepatična neuralgija, dijabetičarska neuropatija, inflamatorni neuropatski bol (trauma), trigeminalana neuralgija ili centralni bol.
22.Jedinjenje za upotrebu prema zahtevu 18, gde je poremećaj posredovan neodgovarajućom aktivnošću PI-3-kinaze astma.
23. Jedinjenje za upotrebu prema zahtevu 18, gde je poremećaj posredovan neodgovarajućom aktivnošću PI3-kinaze COPD.
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Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2280705B1 (en) 2008-06-05 2014-10-08 Glaxo Group Limited Novel compounds
ES2445199T3 (es) * 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
JP5502077B2 (ja) * 2008-06-05 2014-05-28 グラクソ グループ リミテッド 新規な化合物
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
ES2644724T3 (es) 2009-04-30 2017-11-30 Glaxo Group Limited Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas
CN102372675B (zh) * 2010-08-14 2013-12-18 王娜 6-氯-4-碘吲唑及其制备方法与应用
US9102668B2 (en) 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
JP5876051B2 (ja) * 2010-09-08 2016-03-02 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ インフルエンザウィルス感染の治療に使用するためのインダゾール誘導体
HUE026059T2 (en) 2010-09-08 2016-05-30 Glaxosmithkline Ip Dev Ltd N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazol-6-yl ] Polymorphs and salts of 2 - (methyloxy) -3-pyridinyl] methanesulfonamide
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
AU2011326071A1 (en) * 2010-11-08 2013-05-23 Lycera Corporation N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of RORy activity and the treatment of diseases
DK2790705T3 (en) 2011-12-15 2018-03-12 Novartis Ag Use of inhibitors of the activity or function of PI3K
MX367341B (es) 2012-05-08 2019-08-14 Merck Sharp & Dohme Tetrahidronaftiridina y compuestos biciclicos relacionados para la inhibicion de la actividad de rorgamma y el tratamiento de enfermedades.
US9394315B2 (en) 2012-05-08 2016-07-19 Lycera Corporation Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
EP2872143B1 (en) * 2012-07-16 2017-12-13 Neuropore Therapies, Inc. Di-and tri-heteroaryl derivatives as inhibitors of protein aggregation
US20150258127A1 (en) 2012-10-31 2015-09-17 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for preventing antiphospholipid syndrome (aps)
WO2014098232A1 (ja) * 2012-12-21 2014-06-26 Yamashita Chikamasa Ｐｉ３キナーゼ阻害剤を含む医薬組成物、ビタミンｄ受容体に作用する化合物を含む医薬組成物、凍結乾燥組成物、凍結乾燥組成物の製造方法、及び経肺投与用医薬組成物
AU2014336250A1 (en) * 2013-10-17 2016-04-14 Glaxosmithkline Intellectual Property Development Limited PI3K inhibitor for treatment of respiratory disease
US20160263109A1 (en) * 2013-10-17 2016-09-15 Glaxosmithkline Intellectual Property Development Limited P13k inhibitor for treatment of respiratory disease
WO2015095792A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2015095788A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
SG11201605917SA (en) * 2014-01-24 2016-08-30 Abbvie Inc 6-phenyl- or 6-(pyridin-3-yl)indazole derivatives and methods of use
CA2939305A1 (en) 2014-02-27 2015-09-03 Lycera Corporation Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma & related therapeutic methods
US10390989B2 (en) 2014-03-19 2019-08-27 Purewick Corporation Apparatus and methods for receiving discharged urine
US11376152B2 (en) 2014-03-19 2022-07-05 Purewick Corporation Apparatus and methods for receiving discharged urine
US11806266B2 (en) 2014-03-19 2023-11-07 Purewick Corporation Apparatus and methods for receiving discharged urine
US10952889B2 (en) 2016-06-02 2021-03-23 Purewick Corporation Using wicking material to collect liquid for transport
US10226376B2 (en) 2014-03-19 2019-03-12 Purewick Corporation Apparatus and methods for receiving discharged urine
CA2947290A1 (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
WO2015171558A2 (en) 2014-05-05 2015-11-12 Lycera Corporation BENZENESULFONAMIDO AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORγ AND THE TREATEMENT OF DISEASE
US9127069B1 (en) * 2014-06-11 2015-09-08 Antecip Bioventures LLC Compositions comprising rank/rankl antagonists and related compounds for treating pain
CN104086538B (zh) * 2014-06-13 2016-07-06 南京药石科技股份有限公司 一种pi3k激酶抑制剂的中间体及其制备方法与应用
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
CA2975997A1 (en) 2015-02-11 2016-08-18 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as rorgammat inhibitors and uses thereof
JP2018515491A (ja) 2015-05-05 2018-06-14 リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ ＲＯＲγの作動薬及び疾患の療法として使用するジヒドロ−２Ｈ−ベンゾ［ｂ］［１，４］オキサジンスルホンアミド及び関連化合物
GB201509492D0 (en) * 2015-06-02 2015-07-15 Glaxosmithkline Ip Dev Ltd Novel processes
EP3307738B1 (en) 2015-06-11 2022-04-20 The Regents of the University of Michigan Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease
CA3002846A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Substituted bicyclic pyrazole compounds as rorgammat inhibitors and uses thereof
WO2017075185A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
WO2017075182A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Substituted indazole compounds as rorgammat inhibitors and uses thereof
MX2018008272A (es) * 2016-01-14 2019-01-31 Handok Inc Compuestos antagonizantes del receptor a3 de la adenosina, metodo para prepararlos y uso medico de los mismos.
US10376406B2 (en) 2016-07-27 2019-08-13 Purewick Corporation Male urine collection device using wicking material
EP3497100A1 (en) * 2016-08-08 2019-06-19 GlaxoSmithKline Intellectual Property Development Limited Chemical compounds
CA3050918C (en) 2017-01-31 2023-02-14 Purewick Corporation Apparatus and methods for receiving discharged urine
WO2019212955A1 (en) 2018-05-01 2019-11-07 Purewick Corporation Fluid collection devices and methods of using the same
KR102493455B1 (ko) 2018-05-01 2023-01-31 퓨어윅 코포레이션 유체 수집 장치, 관련 시스템 및 관련 방법
KR102491330B1 (ko) 2018-05-01 2023-01-27 퓨어윅 코포레이션 유체 수집 장치, 관련 시스템 및 관련 방법
WO2021138414A1 (en) 2020-01-03 2021-07-08 Purewick Corporation Urine collection devices having a relatively wide portion and an elongated portion and related methods
WO2021211729A1 (en) 2020-04-17 2021-10-21 Purewick Corporation Fluid collection devices, systems, and methods securing a protruding portion in position for use
US12447042B2 (en) 2020-04-17 2025-10-21 Purewick Corporation Fluid collection assemblies including a fluid impermeable barrier having a sump and a base
WO2021211599A1 (en) 2020-04-17 2021-10-21 Purewick Corporation Female external catheter devices having a urethral cup, and related systems and methods
US12491104B2 (en) 2020-04-20 2025-12-09 Purewick Corporation Fluid collection devices adjustable between a vacuum-based orientation and a gravity-based orientation, and related systems and methods
US12048643B2 (en) 2020-05-27 2024-07-30 Purewick Corporation Fluid collection assemblies including at least one inflation device and methods and systems of using the same
US12440371B2 (en) 2020-08-06 2025-10-14 Purewick Corporation Fluid collection system including a garment and a fluid collection device
US20220047410A1 (en) 2020-08-11 2022-02-17 Purewick Corporation Fluid collection assemblies defining waist and leg openings
CA3192236A1 (en) 2020-09-10 2022-03-17 Tony Lahoutte Antibody fragment against fap
US11801186B2 (en) 2020-09-10 2023-10-31 Purewick Corporation Urine storage container handle and lid accessories
US12042423B2 (en) 2020-10-07 2024-07-23 Purewick Corporation Fluid collection systems including at least one tensioning element
US12257174B2 (en) 2020-10-21 2025-03-25 Purewick Corporation Fluid collection assemblies including at least one of a protrusion or at least one expandable material
US12440370B2 (en) 2020-10-21 2025-10-14 Purewick Corporation Apparatus with compressible casing for receiving discharged urine
US12208031B2 (en) 2020-10-21 2025-01-28 Purewick Corporation Adapters for fluid collection devices
US12048644B2 (en) 2020-11-03 2024-07-30 Purewick Corporation Apparatus for receiving discharged urine
US12268627B2 (en) 2021-01-06 2025-04-08 Purewick Corporation Fluid collection assemblies including at least one securement body
CN116940312A (zh) 2021-01-07 2023-10-24 普利维克公司 轮椅固定的尿液收集系统和相关方法
CN115335012A (zh) 2021-01-19 2022-11-11 普利维克公司 可变配合式流体收集设备、系统和方法
EP4274524B1 (en) 2021-02-26 2024-08-28 Purewick Corporation A male fluid collection device configured as a male urine collection device
US12029677B2 (en) 2021-04-06 2024-07-09 Purewick Corporation Fluid collection devices having a collection bag, and related systems and methods
US12251333B2 (en) 2021-05-21 2025-03-18 Purewick Corporation Fluid collection assemblies including at least one inflation device and methods and systems of using the same
US12324767B2 (en) 2021-05-24 2025-06-10 Purewick Corporation Fluid collection assembly including a customizable external support and related methods
US12150885B2 (en) 2021-05-26 2024-11-26 Purewick Corporation Fluid collection system including a cleaning system and methods
JPWO2023127883A1 (me) 2021-12-28 2023-07-06
EP4472638A2 (en) * 2022-01-31 2024-12-11 Intra-Cellular Therapies, Inc. Salt crystals
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
AU2023264245A1 (en) 2022-05-02 2024-12-19 Precirix N.V. Pre-targeting

Family Cites Families (152)

* 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
SK279958B6 (sk) 1992-04-02 1999-06-11 Smithkline Beecham Corporation Zlúčeniny s protialergickým a protizápalovým účink
US5889056A (en) 1994-06-15 1999-03-30 Glaxo Wellsome Inc. Enzyme inhibitors
DE69637257T2 (de) 1995-04-14 2008-06-12 Smithkline Beecham Corp. Verfahren zur Herstellung eines Dosierinhalators
US5821243A (en) 1996-07-22 1998-10-13 Viropharma Incorporated Compounds compositions and methods for treating influenza
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
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
SI1070056T1 (en) 1998-03-14 2004-12-31 Altana Pharma Ag Phthalazinone pde iii/iv inhibitors
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation 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
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. Method and package for storing a pressurized container containing a drug
US6315112B1 (en) 1998-12-18 2001-11-13 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
AU4501800A (en) 1999-05-04 2000-11-17 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
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.
CZ304043B6 (cs) 2000-08-05 2013-09-04 Glaxo Group Limited Estery steroidních thiokyselin
IL155093A0 (en) 2000-09-29 2003-10-31 Glaxo Group Ltd Morpholin-acetamide derivatives for the treatment on inflammatory diseases
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
WO2002067683A1 (en) 2001-02-26 2002-09-06 Merck & Co., Inc. Hiv protease inhibitors supported on cation exchange resins for oral administration
ATE365720T1 (de) 2001-03-08 2007-07-15 Glaxo Group Ltd Agonisten von beta-adrenorezeptoren
WO2002076933A1 (en) 2001-03-22 2002-10-03 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
JP4073786B2 (ja) 2001-04-16 2008-04-09 田辺三菱製薬株式会社 高コンダクタンス型カルシウム感受性ｋチャネル開口薬
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
ES2307751T3 (es) 2001-06-12 2008-12-01 Glaxo Group Limited Nuevos esteres heterociclicos centi-inflamatorios 17 alfa de derivados 17 beta de carbotioato de androstano.
US7498352B2 (en) 2001-06-26 2009-03-03 Takeda Pharmaceutical Company Limited TGF-β superfamily production/secretion promoter
BRPI0212455B8 (pt) 2001-09-14 2021-05-25 Glaxo Group Ltd composto derivado de fenetanolamina para o tratamento de doenças respiratórias, formulação farmacêutica, combinação, e, uso do mesmo
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
WO2003051847A1 (en) 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
JP2005519897A (ja) 2002-01-14 2005-07-07 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、それを含む医薬製剤及びその使用
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
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
EA008830B1 (ru) 2002-03-26 2007-08-31 Бёрингер Ингельхайм Фармасьютиклз, Инк. Миметики глюкокортикоидов, способы их получения, фармацевтические композиции и их применение
WO2003082787A1 (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
ATE496620T1 (de) 2002-04-11 2011-02-15 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
EP1497261B1 (en) 2002-04-25 2007-12-19 Glaxo Group Limited Phenethanolamine derivatives
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
WO2004002480A1 (en) 2002-06-27 2004-01-08 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
DK1521733T3 (da) 2002-07-08 2014-10-13 Pfizer Prod Inc Modulatorer af glucocorticoid receptoren
AU2003251970A1 (en) 2002-07-18 2004-02-09 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
EP1581525A2 (en) 2002-08-09 2005-10-05 AstraZeneca AB Compounds having an activity at metabotropic glutamate receptors
JP2006506340A (ja) 2002-08-09 2006-02-23 アストラゼネカ アクチボラグ 代謝調節型グルタミン酸受容体５のモジュレーターとしてのオキサジアゾール
IL166510A0 (en) 2002-08-09 2006-01-15 Nps Pharma Inc 1,2,4"oxadiazole as modulators of metabotropic glutamate receptor-5
US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
CA2496175A1 (en) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
DE60329193D1 (de) 2002-09-16 2009-10-22 Glaxo Group Ltd Pyrazolo(3,4-b)pyridinverbindungen und ihre verwendung als phosphodiesterasinhibitoren
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
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
HRP20131159B1 (hr) * 2002-09-30 2019-11-01 Bayer Ip Gmbh Taljeni azol-pirimidin derivati
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
WO2004037807A2 (en) 2002-10-22 2004-05-06 Glaxo Group Limited Medicinal arylethanolamine compounds
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
NZ539676A (en) 2002-10-28 2006-10-27 Glaxo Group Ltd Phenethanolamine derivative for the treatment of respiratory diseases
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
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
TW200519106A (en) * 2003-05-02 2005-06-16 Novartis Ag Organic compounds
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
CA2528938A1 (en) 2003-06-13 2005-02-24 Zentaris Gmbh Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
GB0320197D0 (en) * 2003-08-28 2003-10-01 Novartis Ag Organic compounds
SG147436A1 (en) 2003-10-14 2008-11-28 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
EP2468729B1 (en) * 2003-10-15 2013-12-25 Ube Industries, Ltd. Novel indazole derivative
ES2388434T3 (es) 2003-11-03 2012-10-15 Glaxo Group Limited Dispositivo de administración de fluido
TW200524577A (en) 2003-11-04 2005-08-01 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
JP2007514704A (ja) 2003-12-19 2007-06-07 グラクソ　グループ　リミテッド ピラゾロ［３，４−ｂ］ピリジン化合物およびホスホジエステラーゼ阻害剤としてのその使用
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077368A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
US20080227772A1 (en) 2004-02-04 2008-09-18 Neurosearch A/S Diazabicyclic Aryl Derivatives as Nicotinic Acetylcholine Receptor Ligands
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
EP1735314A1 (en) 2004-03-16 2006-12-27 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor
MY144753A (en) 2004-04-27 2011-10-31 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
BRPI0512535A (pt) 2004-06-24 2008-03-25 Incyte Corp compostos de piperidinas n-substituìdas, suas composições e métodos de modulações
WO2006000398A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators
WO2006000401A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited Substituted oxazines as glucocorticoid receptor modulators
US20060013540A1 (en) * 2004-07-19 2006-01-19 Chao Zhang Single fiber optical transceiver module
WO2006135383A2 (en) 2004-08-04 2006-12-21 Myriad Genetics, Inc. Indazoles
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
MX2007004465A (es) 2004-10-19 2007-05-07 Hoffmann La Roche Derivados de quinolina.
CN101103016A (zh) 2004-11-18 2008-01-09 因塞特公司 11-β羟基类固醇脱氢酶1型抑制剂及其使用方法
EP1833787A2 (en) 2004-11-30 2007-09-19 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
ATE517908T1 (de) 2005-01-10 2011-08-15 Glaxo Group Ltd Androstan-17-alpha-carbonat-derivate zur verwendung bei der behandlung allergischer und entzündlicher zustände
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
US7728009B1 (en) 2005-02-18 2010-06-01 Neurogen Corporation Thiazole amides, imidazole amides and related analogues
BRPI0609485A2 (pt) 2005-03-31 2010-04-13 Ronen Kahana criação de aves domésticas e outros animais resistentes a doenças virais
US20060264433A1 (en) 2005-05-23 2006-11-23 Backes Bradley J Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
TW200800946A (en) 2005-08-15 2008-01-01 Astrazeneca Ab Substituted piperazines as metabotropic glutamate receptor antagonists
MX2008002214A (es) 2005-08-16 2008-11-27 Genzyme Corp Compuestos de unión del receptor de quimiocina.
AU2007225836A1 (en) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
EP2007373A4 (en) 2006-03-29 2012-12-19 Foldrx Pharmaceuticals Inc INHIBITION OF ALPHA SYNUCLEINE TOXICITY
MX2008012482A (es) 2006-03-31 2008-10-10 Abbott Lab Compuestos de indazol.
AU2007347115A1 (en) * 2006-04-04 2008-10-23 The Regents Of The University Of California PI3 kinase antagonists
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008020229A2 (en) 2006-08-17 2008-02-21 Astrazeneca Ab Antibacterial pyrrolecarboxamides
TW200824687A (en) 2006-08-25 2008-06-16 Abbott Lab Compounds that inhibit TRPV1 and uses thereof
US7948877B2 (en) * 2006-09-07 2011-05-24 Via Technologies, Inc. Systems and methods for packet forward control
AU2007301607A1 (en) 2006-09-25 2008-04-03 Mutabilis Sa Substituted heterocyclylcarbonylamino-acetic-acid-derivatives as inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘
TWI404532B (zh) 2006-11-02 2013-08-11 Targacept Inc 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
US8450348B2 (en) * 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
JP2010116389A (ja) * 2008-10-17 2010-05-27 Bayer Cropscience Ag 殺虫性アリールピロリジン類
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
US20100210644A1 (en) 2007-06-25 2010-08-19 Boehringer Ingelheim International Gmbh Chemical compounds
US8329897B2 (en) * 2007-07-26 2012-12-11 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
CA2704711C (en) 2007-09-24 2016-07-05 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
JP2009127226A (ja) * 2007-11-21 2009-06-11 Seiji Ohara 温水プールに雪を落し込む手段を持つ融雪装置
PL2300461T3 (pl) 2008-05-01 2013-09-30 Vitae Pharmaceuticals Inc Cykliczne inhibitory dehydrogenazy 11beta-hydroksysteroidów 1
CA2723034A1 (en) * 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8242111B2 (en) * 2008-05-01 2012-08-14 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
US8569292B2 (en) * 2008-05-01 2013-10-29 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
ES2445199T3 (es) * 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
ES2566339T3 (es) 2008-06-05 2016-04-12 Glaxo Group Limited Derivados de 4-carboxamida indazol útiles como inhibidores de PI3-quinasas
EP2280705B1 (en) * 2008-06-05 2014-10-08 Glaxo Group Limited Novel compounds
JP5502077B2 (ja) * 2008-06-05 2014-05-28 グラクソ グループ リミテッド 新規な化合物
WO2009150976A1 (ja) * 2008-06-11 2009-12-17 浜松ホトニクス株式会社 ガラス溶着方法
JP5379160B2 (ja) * 2008-07-25 2013-12-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
US8245111B2 (en) * 2008-12-09 2012-08-14 Intel Corporation Performing multi-bit error correction on a cache line
WO2010068287A2 (en) 2008-12-11 2010-06-17 Angion Biomedica Corp. Small molecule modulators of hepatocyte growth factor (scatter factor) activity
US20120039905A1 (en) 2009-01-13 2012-02-16 The Babraham Institute The Role of p110 delta Signaling in Morbidity and Lung Pathology Induced by Influenza Virus Infection
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
US8343959B2 (en) * 2009-04-30 2013-01-01 Abbott Gmbh & Co. Kg N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
GEP20156309B (en) 2009-04-30 2015-07-10 Vitae Pharmaceuticals Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2424838A1 (en) * 2009-04-30 2012-03-07 Bayer CropScience AG Pesticidal arylpyrrolidines
MA33216B1 (fr) * 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
EP2432769B1 (en) * 2009-04-30 2015-04-01 AbbVie Deutschland GmbH & Co KG N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor
ES2644724T3 (es) 2009-04-30 2017-11-30 Glaxo Group Limited Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas
US20120238571A1 (en) * 2009-12-03 2012-09-20 Glaxo Group Limited Indazole derivatives as pi 3-kinase
JP2013512879A (ja) 2009-12-03 2013-04-18 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
EP2507226A1 (en) * 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
US9102668B2 (en) 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
JP5876051B2 (ja) 2010-09-08 2016-03-02 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ インフルエンザウィルス感染の治療に使用するためのインダゾール誘導体
HUE026059T2 (en) 2010-09-08 2016-05-30 Glaxosmithkline Ip Dev Ltd N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazol-6-yl ] Polymorphs and salts of 2 - (methyloxy) -3-pyridinyl] methanesulfonamide
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
US10642898B1 (en) * 2017-04-11 2020-05-05 Northrop Grumman Systems Corporation Three-dimensional graph

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