EA201390457A1 - Полиморфы и соли 6-(1h-индол-4-ил)-4-(5-{[4-(1-метилэтил)-1-пиперазинил]метил}-1,3-оксазол-2-ил)-1h-индазола в качестве ингибиторов pi3k для применения в лечении, например, респираторных расстройств - Google Patents

Полиморфы и соли 6-(1h-индол-4-ил)-4-(5-{[4-(1-метилэтил)-1-пиперазинил]метил}-1,3-оксазол-2-ил)-1h-индазола в качестве ингибиторов pi3k для применения в лечении, например, респираторных расстройств

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Publication number
EA201390457A1
EA201390457A1 EA201390457A EA201390457A EA201390457A1 EA 201390457 A1 EA201390457 A1 EA 201390457A1 EA 201390457 A EA201390457 A EA 201390457A EA 201390457 A EA201390457 A EA 201390457A EA 201390457 A1 EA201390457 A1 EA 201390457A1
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EA
Eurasian Patent Office
Prior art keywords
salts
piperasinyl
polymorphes
oxazol
indazole
Prior art date
Application number
EA201390457A
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English (en)
Other versions
EA022872B1 (ru
Inventor
Джули Николь Хэмблин
Пол Спенсер Джонс
Сюзанн Элейн Килинг
Джоэль Ли
Найджел Джеймс Парр
Роберт Дэвид Уиллэси
Original Assignee
Глаксо Груп Лимитед
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Application filed by Глаксо Груп Лимитед filed Critical Глаксо Груп Лимитед
Publication of EA201390457A1 publication Critical patent/EA201390457A1/ru
Publication of EA022872B1 publication Critical patent/EA022872B1/ru

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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Abstract

Настоящее изобретение относится к полиморфу соединения формулы (II), которое является ингибитором активности киназы PI3, и его солям и их полиморфам.
EA201390457A 2010-10-27 2011-10-25 Гемисукцинатная соль 6-(1h-индол-4-ил)-4-(5-{[4-(1-метилэтил)-1-пиперазинил]метил}-1,3-оксазол-2-ил)-1h-индазола, ее полиморф, содержащая их фармацевтическая композиция, их применение и способ лечения EA022872B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1018124.6A GB201018124D0 (en) 2010-10-27 2010-10-27 Polymorphs and salts
PCT/EP2011/068604 WO2012055846A1 (en) 2010-10-27 2011-10-25 Polymorphs and salts of 6-(1h-indol-4-yl)-4-(5- { [4-(1-methylethyl)-1-pi perazinyl] methyl} -1,3-oxazol-2-yl)-1h-indazole as pi3k inhibitors for use in the treatment of e.g. respiratory disorders

Publications (2)

Publication Number Publication Date
EA201390457A1 true EA201390457A1 (ru) 2013-11-29
EA022872B1 EA022872B1 (ru) 2016-03-31

Family

ID=43365584

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201390457A EA022872B1 (ru) 2010-10-27 2011-10-25 Гемисукцинатная соль 6-(1h-индол-4-ил)-4-(5-{[4-(1-метилэтил)-1-пиперазинил]метил}-1,3-оксазол-2-ил)-1h-индазола, ее полиморф, содержащая их фармацевтическая композиция, их применение и способ лечения

Country Status (26)

Country Link
US (1) US8993576B2 (ru)
EP (2) EP2632921B1 (ru)
JP (1) JP5894603B2 (ru)
KR (1) KR101774026B1 (ru)
CN (1) CN103270037B (ru)
AU (1) AU2011322649B2 (ru)
BR (1) BR112013010126B1 (ru)
CA (1) CA2814436C (ru)
CY (1) CY1121248T1 (ru)
DK (1) DK2632921T3 (ru)
EA (1) EA022872B1 (ru)
ES (1) ES2703716T3 (ru)
GB (1) GB201018124D0 (ru)
HR (1) HRP20182059T1 (ru)
HU (1) HUE042754T2 (ru)
IL (1) IL225704A (ru)
LT (1) LT2632921T (ru)
MX (1) MX347619B (ru)
PL (1) PL2632921T3 (ru)
PT (1) PT2632921T (ru)
RS (1) RS58072B1 (ru)
SG (1) SG189179A1 (ru)
SI (1) SI2632921T1 (ru)
TR (1) TR201819939T4 (ru)
WO (1) WO2012055846A1 (ru)
ZA (1) ZA201302480B (ru)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2445199T3 (es) 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
US8536169B2 (en) 2008-06-05 2013-09-17 Glaxo Group Limited Compounds
ES2383246T3 (es) 2008-06-05 2012-06-19 Glaxo Group Limited 4-amino-indazoles
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
US8575162B2 (en) 2009-04-30 2013-11-05 Glaxosmithkline Intellectual Property Development Limited Compounds
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
EP2878594B1 (en) * 2012-07-27 2018-11-28 Sato Pharmaceutical Co., Ltd. Difluoromethylene compound
EP2916868B1 (en) 2012-11-08 2022-05-11 Rhizen Pharmaceuticals S.A. Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor
US20160256466A1 (en) * 2013-10-17 2016-09-08 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
CA2925064A1 (en) * 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
GB201509492D0 (en) * 2015-06-02 2015-07-15 Glaxosmithkline Ip Dev Ltd Novel processes

Family Cites Families (138)

* 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
WO1993019749A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
AU692892B2 (en) 1994-06-15 1998-06-18 Wellcome Foundation Limited, The Enzyme inhibitors
JPH11509433A (ja) 1995-04-14 1999-08-24 グラクソ、ウェルカム、インコーポレーテッド アルブテロール用計量投与用吸入器
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 (fr) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Derives de benzodioxole
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
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. 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
US6352152B1 (en) 1998-12-18 2002-03-05 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
CN1353717A (zh) 1999-05-04 2002-06-12 莱加制药公司 四环黄体酮受体调节剂化合物及其方法
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.
EA005992B1 (ru) 2000-08-05 2005-08-25 Глаксо Груп Лимитед S-ФТОРМЕТИЛОВЫЙ ЭФИР 6α,9α-ДИФТОР-17α-[(2-ФУРАНИЛКАРБОНИЛ)ОКСИ]-11β-ГИДРОКСИ-16α-МЕТИЛ-3-ОКСОАНДРОСТА-1,4-ДИЕН-17β-КАРБОТИОКИСЛОТЫ В КАЧЕСТВЕ ПРОТИВОВОСПАЛИТЕЛЬНОГО АГЕНТА
MXPA03002814A (es) 2000-09-29 2003-10-14 Glaxo Group Ltd 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
WO2002067683A1 (en) 2001-02-26 2002-09-06 Merck & Co., Inc. Hiv protease inhibitors supported on cation exchange resins for oral administration
US7144908B2 (en) 2001-03-08 2006-12-05 Glaxo Group Limited Agonists of beta-adrenoceptors
US7045658B2 (en) 2001-03-22 2006-05-16 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
PL367325A1 (en) 2001-04-16 2005-02-21 Tanabe Seiyaku Co, Ltd. Large conductance calcium-activated k channel opener
AU2002253342B2 (en) 2001-04-30 2007-01-04 Glaxo Group Limited Novel anti-inflammatory androstane derivatives
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.
WO2003000257A1 (fr) 2001-06-26 2003-01-03 Takeda Chemical Industries, Ltd. Promoteur de production/secretion de la superfamille des tgf-$g(b)
ES2316599T3 (es) 2001-09-14 2009-04-16 Glaxo Group Limited Derivados de fenetanolamina para el tratamiento de enfermedades respiratorias.
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 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
WO2003059899A1 (en) 2002-01-14 2003-07-24 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof
AU2003214879B2 (en) 2002-01-22 2008-02-07 The Regents Of The University Of California Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof
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
AU2003230700A1 (en) 2002-03-26 2003-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
UA80120C2 (en) 2002-03-26 2007-08-27 Boehringer Ingelheim Pharma Glucocorticoid mimetics, pharmaceutical composition based thereon
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
DE60335869D1 (de) 2002-04-11 2011-03-10 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
ES2298511T3 (es) 2002-04-25 2008-05-16 Glaxo Group Limited Derivados de fenetanolamina.
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
AU2003233780A1 (en) 2002-06-27 2004-01-19 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
MXPA05000345A (es) 2002-07-08 2005-03-31 Pfizer Prod Inc Moduladores del receptor de glucocorticoides.
PL375442A1 (en) 2002-07-18 2005-11-28 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
WO2004014902A2 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
UA87653C2 (en) 2002-08-09 2009-08-10 Астразенека Аб 1,2,4-oxadiazols as modulators of receptor-5 for metabotropic glutamate
EP1536790A2 (en) 2002-08-09 2005-06-08 AstraZeneca AB Oxadiazoles 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
ES2331119T3 (es) 2002-09-16 2009-12-22 Glaxo Group Limited Compuestos de pirazolo(3,4-b)piridina, y su uso como inhibidores de fosfodiesterasa.
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
AU2003270783C1 (en) 2002-09-20 2010-05-20 Merck Sharp & Dohme Corp. Octahydro-2-H-naphtho[1,2-F] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
US20060205790A1 (en) 2002-10-22 2006-09-14 Coe Diane M Medicinal arylethanolamine compounds
KR20050057681A (ko) 2002-10-28 2005-06-16 글락소 그룹 리미티드 호흡기 질환의 치료에 유용한 페네탄올아민 유도체
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
CN1823067A (zh) 2003-06-13 2006-08-23 赞塔里斯有限公司 具有抑制磷脂酰肌醇3－激酶活性的化合物及其使用方法
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
AP2007004239A0 (en) 2003-10-14 2007-12-31 Glaxo Group Ltd Muscarinic acetycholine receptor antagonists
TWI344961B (en) 2003-10-15 2011-07-11 Ube Industries Novel indazole derivative
BRPI0416128B8 (pt) 2003-11-03 2021-06-22 Glaxo Group Ltd dispositivo de dispensação de fluido
PE20050489A1 (es) 2003-11-04 2005-09-02 Glaxo Group Ltd Antagonistas de receptores de acetilcolina muscarinicos
US20070111995A1 (en) 2003-12-19 2007-05-17 Allen David G Pyrazolo [3,4-B] pyridine Compounds and Their Use as Phosphodiesterase Inhibitors
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077368A2 (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
JP2007520527A (ja) 2004-02-04 2007-07-26 ノイロサーチ アクティーゼルスカブ ニコチン性アセチルコリン受容体リガンドとしてのジアザ２環式アリール誘導体
BRPI0508843A (pt) 2004-03-16 2007-08-28 Glaxo Group Ltd composto ou sal do mesmo, método para preparar um composto ou um sal do mesmo, método de tratamento e/ou profilaxia de doença, e, composição farmacêutica
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
PE20060259A1 (es) 2004-04-27 2006-03-25 Glaxo Group Ltd Compuestos de quinuclidina como antagonistas del receptor de acetilcolina muscarinico
EP1758580A4 (en) 2004-06-24 2008-01-16 Incyte Corp N-SUBSTITUTED PIPERIDINE AND ITS USE AS A MEDICAMENT
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
EP1805166B1 (en) 2004-10-19 2011-07-27 F. Hoffmann-La Roche AG Quinoline derivatives
CA2587153A1 (en) 2004-11-18 2006-05-26 Incyte Corporation Inhibitors of 11-.beta. hydroxyl steroid dehydrogenase type 1 and methods of using the same
JP2008521831A (ja) 2004-11-30 2008-06-26 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
WO2006072599A2 (en) 2005-01-10 2006-07-13 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
WO2006089076A2 (en) 2005-02-18 2006-08-24 Neurogen Corporation Thiazole amides, imidazole amides and related analogues
US20060264433A1 (en) 2005-05-23 2006-11-23 Backes Bradley J Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
WO2007011759A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
TW200800946A (en) 2005-08-15 2008-01-01 Astrazeneca Ab Substituted piperazines as metabotropic glutamate receptor antagonists
CA2619881A1 (en) 2005-08-16 2007-02-22 Genzyme Corporation Chemokine receptor binding compounds
CN101443322A (zh) 2006-03-10 2009-05-27 小野药品工业株式会社 含氮杂环衍生物及含有该衍生物作为活性成分的药物
JP2009531443A (ja) 2006-03-29 2009-09-03 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド α−シヌクレイン毒性の抑制
PT2004654E (pt) 2006-04-04 2013-08-27 Univ California Derivados de pirazolopirimidina para utilização como antagonistas da quinase
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
ATE553093T1 (de) 2006-08-25 2012-04-15 Abbott Lab Indazolderivate zur hemmung von trpv1 und verwendungen davon
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
WO2008037477A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as p13k lipid kinase inhibitors
TWI454262B (zh) 2006-11-02 2014-10-01 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
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
JP5451611B2 (ja) 2007-07-26 2014-03-26 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１のサイクリックインヒビター
JP5451752B2 (ja) 2008-05-01 2014-03-26 ヴァイティー ファーマシューティカルズ，インコーポレイテッド 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
EP2291371B1 (en) 2008-05-01 2015-06-10 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5538365B2 (ja) 2008-05-01 2014-07-02 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
EP2300461B1 (en) 2008-05-01 2013-04-17 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8536169B2 (en) 2008-06-05 2013-09-17 Glaxo Group Limited Compounds
WO2009147187A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited 4-carboxamide indazole derivatives useful as inhibitors of p13-kinases
ES2445199T3 (es) 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
ES2383246T3 (es) 2008-06-05 2012-06-19 Glaxo Group Limited 4-amino-indazoles
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
WO2010127237A2 (en) 2009-04-30 2010-11-04 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2687525B1 (en) 2008-07-25 2015-09-23 Boehringer Ingelheim International GmbH Cyclic inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
US20110237633A1 (en) 2008-12-11 2011-09-29 Bijoy Panicker Small molecule modulators of hepatocyte growth factor (scatter factor) activity
EP2963116B1 (en) 2009-03-04 2020-11-11 CuRNA, Inc. Treatment of sirtuin 1 (sirt1) related diseases by inhibition of natural antisense transcript to sirt 1
US8524751B2 (en) * 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
US8575162B2 (en) 2009-04-30 2013-11-05 Glaxosmithkline Intellectual Property Development Limited Compounds
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
SG175187A1 (en) 2009-04-30 2011-11-28 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
WO2010124845A1 (en) 2009-04-30 2010-11-04 Bayer Cropscience Ag Pesticidal arylpyrrolidines
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
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
WO2011067366A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
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
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
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

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