KR102038462B1 - Pi3k의 활성 또는 기능의 억제제의 용도 - Google Patents

Pi3k의 활성 또는 기능의 억제제의 용도 Download PDF

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KR102038462B1
KR102038462B1 KR1020147019204A KR20147019204A KR102038462B1 KR 102038462 B1 KR102038462 B1 KR 102038462B1 KR 1020147019204 A KR1020147019204 A KR 1020147019204A KR 20147019204 A KR20147019204 A KR 20147019204A KR 102038462 B1 KR102038462 B1 KR 102038462B1
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pyrrolidin
methoxy
yloxy
pyridin
tetrahydro
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KR20140107421A (ko
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나이젤 그라함 쿡
파울로 안토니오 페르난데스 고메즈 도스 산토스
파스칼 푸렛
크리스티나 허바흐
클레멘스 회게나우어
그레고리 홀링스워스
크리스토프 칼리스
이안 루이스
알렉산더 백스터 스미스
니콜라스 솔더만
프레드릭 스타우페르
로스 스트랑
프랑크 스토바서
니콜라 투필리
아네트 폰 매트
로메인 울프
프레드릭 제크리
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노파르티스 아게
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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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
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    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • AHUMAN NECESSITIES
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    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
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    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Steroid Compounds (AREA)
KR1020147019204A 2011-12-15 2012-12-14 Pi3k의 활성 또는 기능의 억제제의 용도 Active KR102038462B1 (ko)

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Application Number Priority Date Filing Date Title
US201161576194P 2011-12-15 2011-12-15
US61/576,194 2011-12-15
PCT/IB2012/057332 WO2013088404A1 (en) 2011-12-15 2012-12-14 Use of inhibitors of the activity or function of PI3K

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KR20140107421A KR20140107421A (ko) 2014-09-04
KR102038462B1 true KR102038462B1 (ko) 2019-10-31

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EP (1) EP2790705B1 (enExample)
JP (1) JP6117235B2 (enExample)
KR (1) KR102038462B1 (enExample)
CN (1) CN103998042B (enExample)
AP (1) AP3849A (enExample)
AU (1) AU2012354094C1 (enExample)
BR (1) BR112014014327A2 (enExample)
CA (1) CA2857302C (enExample)
DK (1) DK2790705T3 (enExample)
EA (1) EA029473B1 (enExample)
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PH (1) PH12014501348A1 (enExample)
PL (1) PL2790705T3 (enExample)
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SI (1) SI2790705T1 (enExample)
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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
CA2857302C (en) 2011-12-15 2020-08-25 Novartis Ag Use of inhibitors of the activity or function of pi3k
AU2013343291B2 (en) 2012-11-07 2018-05-10 Karus Therapeutics Ltd Novel histone deacetylase inhibitors and their use in therapy
EP2994465B1 (en) 2013-05-10 2018-08-15 Karus Therapeutics Limited Novel histone deacetylase inhibitors
US20150105383A1 (en) * 2013-10-10 2015-04-16 Acetylon Pharmaceuticals, Inc. HDAC Inhibitors, Alone Or In Combination With PI3K Inhibitors, For Treating Non-Hodgkin's Lymphoma
US9908872B2 (en) 2013-12-13 2018-03-06 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
JP6879740B2 (ja) 2013-12-13 2021-06-02 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド リンパ形質細胞性リンパ腫を処置する方法
WO2015162584A1 (en) 2014-04-24 2015-10-29 Novartis Ag Crystalline forms of the sulfate salt of n-[5-(3-imidazol-1-yl-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]-acetamide
JP6788583B2 (ja) 2014-10-22 2020-11-25 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド 増殖性疾患を処置するためのチアゾリル含有化合物
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
TWI903299B (zh) 2018-03-08 2025-11-01 美商英塞特公司 作為PI3K-γ抑制劑之胺基吡嗪二醇化合物
US20220106296A1 (en) * 2018-06-19 2022-04-07 Novartis Ag Cyanotriazole compounds and uses thereof
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
EP3825303A4 (en) 2018-07-17 2022-07-06 Nippon Chemiphar Co., Ltd. T-type calcium channel blocker
CA3135344A1 (en) 2019-03-29 2020-10-08 Nippon Chemiphar Co., Ltd. Use of t-type calcium channel blocker for treating pruritus
AU2023232562A1 (en) 2022-03-08 2024-09-05 Equashield Medical Ltd Fluid transfer station in a robotic pharmaceutical preparation system
CN114957676B (zh) * 2022-06-22 2023-05-16 安徽工程大学 一种利用反溶剂沉积快速调控水分活度制备美拉德反应产物的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005086814A2 (en) * 2004-03-09 2005-09-22 The Uab Research Foundation Methods and compositions related to regulation of cytokine production by glycogen synthase kinase 3 (gsk-3)
WO2010129816A2 (en) * 2009-05-07 2010-11-11 Intellikine, Inc. Heterocyclic compounds and uses thereof

Family Cites Families (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5300645A (en) 1993-04-14 1994-04-05 Eli Lilly And Company Tetrahydro-pyrido-indole
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
US5939421A (en) 1997-07-01 1999-08-17 Signal Pharmaceuticals, Inc. Quinazoline analogs and related compounds and methods for treating inflammatory conditions
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
WO2001085986A2 (en) 2000-05-10 2001-11-15 Icos Corporation Phosphatidyl inositol 3-kinase delta binding partner
DE10043667A1 (de) 2000-09-05 2002-03-14 Merck Patent Gmbh 2-Guanidino-4-aryl-chinazoline
ES2332770T3 (es) 2000-11-07 2010-02-12 Novartis Ag Derivados de indolilmaleimida como inhibidores de la proteina quinasa c.
JP3836436B2 (ja) 2001-04-27 2006-10-25 全薬工業株式会社 複素環式化合物及びそれを有効成分とする抗腫瘍剤
PE20040079A1 (es) 2002-04-03 2004-04-19 Novartis Ag Derivados de indolilmaleimida
EP1578411A4 (en) 2002-12-09 2007-05-02 Univ Texas PROCESS FOR THE SELECTIVE INHIBITION OF JANUS TYROSINE KINASE3 (JAK3)
MXPA05007010A (es) 2002-12-27 2005-08-18 Angeletti P Ist Richerche Bio Tetrahidro-4h-pirido[1,2-a]pirimidinas y compuestos relacionados utiles como inhibidores de la integrasa del virus de inmunodeficiencia humana.
WO2005016349A1 (en) 2003-08-14 2005-02-24 Icos Corporation Methods of inhibiting leukocyte accumulation
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
DK1704145T3 (da) 2004-01-12 2012-09-24 Ym Biosciences Australia Pty Selektive kinaseinhibitorer
CA2553969A1 (en) 2004-01-23 2005-08-04 Amgen Inc. Vanilloid receptor ligands and their use in treatments
PL1761540T3 (pl) 2004-05-13 2017-06-30 Icos Corporation Chinazolinony jako inhibitory ludzkiej kinazy 3-fosfatydyloinozytolu delta
CA2566436C (en) 2004-05-13 2011-05-10 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
JP4163738B2 (ja) 2004-06-11 2008-10-08 日本たばこ産業株式会社 癌の治療用の5−アミノ−2,4,7−トリオキソ−3,4,7,8−テトラヒドロ−2H−ピリド’2,3−d!ピリミジン誘導体及び関連化合物
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
JP2008526734A (ja) 2004-12-31 2008-07-24 エスケー ケミカルズ カンパニー リミテッド 糖尿及び肥満治療予防に有効なキナゾリン誘導体
CA2606760C (en) 2005-05-04 2014-12-23 Renovis, Inc. Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds and compositions thereof useful in the treatment of conditions associated with neurological and inflammatory disorders and disfunctions
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2007023186A1 (en) 2005-08-26 2007-03-01 Laboratoires Serono S.A. Pyrazine derivatives and use as pi3k inhibitors
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
WO2007071055A1 (en) 2005-12-21 2007-06-28 Painceptor Pharma Corporation Compositions and methods for modulating gated ion channels
GB0612630D0 (en) 2006-06-26 2006-08-02 Novartis Ag Organic compounds
US8673929B2 (en) 2006-07-20 2014-03-18 Gilead Sciences, Inc. 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections
AU2007278178A1 (en) * 2006-07-28 2008-01-31 Novartis Ag 2,4-substituted quinazolines as lipid kinase inhibitors
EP1891958A1 (en) 2006-08-03 2008-02-27 Universite Pierre Et Marie Curie (Paris Vi) Rho/Rock/PI3/Akt kinase inhibitors for the treatment of diseases associated with protozoan parasites.
SG178786A1 (en) 2006-11-13 2012-03-29 Lilly Co Eli Thienopyrimidinones for treatment of inflammatory disorders and cancers
US7705018B2 (en) 2007-03-23 2010-04-27 Amgen Inc. Substituted quinolines and their uses in treatment of inflammatory and related conditions
AU2008231304B2 (en) 2007-03-23 2011-05-12 Amgen Inc. Heterocyclic compounds and their uses
EP2132207A2 (en) 2007-03-23 2009-12-16 Amgen Inc. Heterocyclic compounds and their uses
EP2136639B1 (en) 2007-04-02 2016-03-09 Evotec AG Pyrid-2-yl fused heterocyclic compounds, and compositions and uses thereof
CA2683624A1 (en) 2007-04-12 2008-10-23 F. Hoffmann-La Roche Ag Pharmaceutical compounds
WO2008125833A1 (en) 2007-04-12 2008-10-23 Piramed Limited Pharmaceutical compounds
GB0707087D0 (en) 2007-04-12 2007-05-23 Piramed Ltd Pharmaceutical compounds
US8076345B2 (en) 2007-04-17 2011-12-13 Evotec Ag 2-cyanophenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine compounds, compositions and uses thereof
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
WO2008150827A1 (en) 2007-05-29 2008-12-11 Smithkline Beecham Corporation Naphthyridine, derivatives as p13 kinase inhibitors
EP2158207B1 (en) 2007-06-12 2011-05-25 F. Hoffmann-La Roche AG Thiazoliopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase
WO2008152387A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Quinazoline derivatives as pi3 kinase inhibitors
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
UY31137A1 (es) * 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
RU2341527C1 (ru) 2007-07-17 2008-12-20 Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" Аннелированные азагетероциклы, включающие пиримидиновый фрагмент, способ их получения и ингибиторы pi3k киназ
TW200908984A (en) 2007-08-07 2009-03-01 Piramal Life Sciences Ltd Pyridyl derivatives, their preparation and use
WO2009036768A2 (en) 2007-09-19 2009-03-26 H. Lundbeck A/S Diagnosing potential weight gain in a subject
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
US20100298289A1 (en) 2007-10-09 2010-11-25 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
WO2009058361A1 (en) * 2007-10-31 2009-05-07 Dynavax Technologies Corp. Inhibition of type i ifn production
NZ585460A (en) 2007-11-13 2013-02-22 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
AU2009204483B2 (en) 2008-01-04 2014-03-13 Intellikine, Llc Certain chemical entities, compositions and methods
US20110053907A1 (en) 2008-03-27 2011-03-03 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
US8436005B2 (en) 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
WO2009147189A1 (en) 2008-06-05 2009-12-10 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
KR20110018451A (ko) 2008-06-19 2011-02-23 밀레니엄 파머슈티컬스 인코퍼레이티드 티오펜 또는 티아졸 유도체, 그리고 pi3k 저해물질로서 이들의 용도
CA2730271A1 (en) 2008-07-07 2010-01-14 Xcovery Holding Company Llc Pi3k isoform selective inhibitors
MX2011000216A (es) 2008-07-08 2011-03-29 Intellikine Inc Inhibidores de cinasa y metodos para su uso.
WO2010036908A1 (en) * 2008-09-26 2010-04-01 Eisai R & D Management Co., Ltd. Use of benzoxazole compounds in the treatment of malaria
WO2010036380A1 (en) 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
NZ631024A (en) 2008-11-13 2016-04-29 Gilead Calistoga Llc Therapies for hematologic malignancies
US20110269779A1 (en) 2008-11-18 2011-11-03 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
US20110294803A1 (en) 2008-12-04 2011-12-01 Law Amanda J Phosphatidylinositol-3-kinase p110 delta-targeted drugs in the treatment of cns disorders
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
US8293783B2 (en) 2009-03-24 2012-10-23 National University Of Singapore Use of artemisinin derivatives for the treatment of asthma and chronic obstructive pulmonary disease (COPD)
SG174529A1 (en) 2009-03-24 2011-10-28 Gilead Calistoga Llc Atropisomers of2-purinyl-3-tolyl-quinazolinone derivatives and methods of use
WO2010120991A1 (en) * 2009-04-17 2010-10-21 Wyeth Llc 5, 6, 7, 8-tetrahydropyrido[4,3-d]pyrimidine compounds, their use as mtor, pi3, and hsmg-1 kinase inhibitors, and their syntheses
PT2421536E (pt) 2009-04-20 2015-10-20 Gilead Calistoga Llc Métodos de tratamento para tumores sólidos
CN102459253B (zh) 2009-04-30 2015-03-25 葛兰素集团有限公司 作为pi3-激酶抑制剂的*唑取代的吲唑化合物
US8173650B2 (en) 2009-05-27 2012-05-08 Genentech, Inc. Bicyclic pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use
WO2010136491A1 (en) 2009-05-27 2010-12-02 F. Hoffmann-La Roche Ag Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
US8754089B2 (en) 2009-06-25 2014-06-17 Amgen Inc. Heterocyclic compounds and their uses
MX2011013666A (es) 2009-06-25 2012-03-06 Amgen Inc Compuestos heterociclicos y sus usos.
JP2012531436A (ja) 2009-06-25 2012-12-10 アムジエン・インコーポレーテツド 複素環式化合物およびそれらのpi3k活性阻害剤としての使用
UY32743A (es) 2009-06-25 2010-12-31 Amgen Inc Compuestos heterocíclicos y sus usos
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
HUE034503T2 (en) 2009-07-02 2018-02-28 Sanofi Sa 2,3-Dihydro-1-imidazo [1,2-a] pyrimidin-5-one derivatives, their preparation process and their use in medicine
ES2487623T3 (es) 2009-07-02 2014-08-22 Sanofi Derivados de 6,7,8,9-tetrahidro-pirimido{1,2-a}pirimidin-4-ona, su preparación y su aplicación farmacéutica
EP2456443A1 (en) 2009-07-21 2012-05-30 Gilead Calistoga LLC Treatment of liver disorders with pi3k inhibitors
JP5746172B2 (ja) 2009-08-20 2015-07-08 カルス セラピューティクス リミテッド ホスホイノシチド3−キナーゼ阻害剤としての三環式複素環化合物
WO2011041399A2 (en) 2009-09-29 2011-04-07 Tyrogenex, Inc. Pi3k (delta) selective inhibitors
GB0918249D0 (en) 2009-10-19 2009-12-02 Respivert Ltd Compounds
PT2496567T (pt) 2009-11-05 2017-11-15 Rhizen Pharmaceuticals S A Novos moduladores de quinase benzopiran
EP2496577A1 (en) 2009-11-06 2012-09-12 Piramal Life Sciences Limited Imidazopyridine derivatives
MX2012005518A (es) 2009-11-13 2012-06-19 Merck Serono Sa Derivados de pirazol amina triciclica.
EP2507223A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
WO2011067366A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
US20120238559A1 (en) 2009-12-03 2012-09-20 Glaxo Group Limited Novel compounds
EP2513109A1 (en) 2009-12-18 2012-10-24 Amgen Inc. Heterocyclic compounds and their uses
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
AR079529A1 (es) 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
EP2539337A1 (en) 2010-02-22 2013-01-02 F. Hoffmann-La Roche AG Pyrido[3,2-d]pyrimidine pi3k delta inhibitor compounds and methods of use
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
GB201007347D0 (en) 2010-04-30 2010-06-16 Karus Therapeutics Ltd Compounds
JP5951600B2 (ja) 2010-05-21 2016-07-13 インフィニティー ファーマシューティカルズ, インコーポレイテッド キナーゼ調節のための、化合物、組成物および方法
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
CA2802808A1 (en) 2010-07-14 2012-01-19 F. Hoffmann-La Roche Ag Purine compounds selective for pi3k p110 delta, and methods of use
JP5954838B2 (ja) 2010-09-14 2016-07-20 エクセリクシス, インク. Pi3k−デルタの阻害剤ならびにそれらの使用法および製造法
TWI642670B (zh) 2010-09-14 2018-12-01 伊塞利克斯公司 Pi3k-德爾塔抑制劑以及其應用和生產方法
KR20180080358A (ko) 2011-01-10 2018-07-11 인피니티 파마슈티칼스, 인코포레이티드 이소퀴놀린온 및 이의 고체 형태의 제조 방법
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
MX340013B (es) 2011-03-21 2016-06-22 Hoffmann La Roche Compuestos de benzoxazepina selectivos para fosfatidilinositol 3-cinasa (pi3k) p110 delta y metodos de uso.
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
BR112013024909A2 (pt) 2011-03-28 2019-09-24 Mei Pharma Inc composto, composição farmacêutica, método para o tratamento, prevenção ou melhoria de um ou mais sintomas de desordem, doença, ou condição mediada por pi3k, e método para modular a atividade enzimática de pi3k
US8530470B2 (en) 2011-04-13 2013-09-10 Astrazeneca Ab Chromenone derivatives
EP2518071A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Imidazopyridine derivatives as PI3K inhibitors
EP2518070A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
WO2013057711A1 (en) * 2011-10-21 2013-04-25 Novartis Ag Quinazoline derivatives as pi3k modulators
CA2857302C (en) 2011-12-15 2020-08-25 Novartis Ag Use of inhibitors of the activity or function of pi3k

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005086814A2 (en) * 2004-03-09 2005-09-22 The Uab Research Foundation Methods and compositions related to regulation of cytokine production by glycogen synthase kinase 3 (gsk-3)
WO2010129816A2 (en) * 2009-05-07 2010-11-11 Intellikine, Inc. Heterocyclic compounds and uses thereof

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