JP2013530236A - Pi3k活性の阻害剤としての複素環式化合物およびその用途 - Google Patents

Pi3k活性の阻害剤としての複素環式化合物およびその用途 Download PDF

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JP2013530236A
JP2013530236A JP2013518683A JP2013518683A JP2013530236A JP 2013530236 A JP2013530236 A JP 2013530236A JP 2013518683 A JP2013518683 A JP 2013518683A JP 2013518683 A JP2013518683 A JP 2013518683A JP 2013530236 A JP2013530236 A JP 2013530236A
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ルーカス,ブライアン
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アムジエン・インコーポレーテツド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2013518683A 2010-07-01 2011-06-30 Pi3k活性の阻害剤としての複素環式化合物およびその用途 Withdrawn JP2013530236A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36074310P 2010-07-01 2010-07-01
US61/360,743 2010-07-01
PCT/US2011/042499 WO2012003262A1 (en) 2010-07-01 2011-06-30 Heterocyclic compounds and their use as inhibitors of pi3k activity

Publications (2)

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JP2013530236A true JP2013530236A (ja) 2013-07-25
JP2013530236A5 JP2013530236A5 (enExample) 2014-08-14

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JP2013518683A Withdrawn JP2013530236A (ja) 2010-07-01 2011-06-30 Pi3k活性の阻害剤としての複素環式化合物およびその用途

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Country Link
US (1) US8759371B2 (enExample)
EP (1) EP2588468B1 (enExample)
JP (1) JP2013530236A (enExample)
AU (1) AU2011271460B2 (enExample)
CA (1) CA2803259A1 (enExample)
ES (1) ES2472720T3 (enExample)
MX (1) MX2012014996A (enExample)
WO (1) WO2012003262A1 (enExample)

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EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
MX389479B (es) 2011-09-02 2025-03-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k)
US20150011569A1 (en) * 2011-12-15 2015-01-08 Philadelphia Health & Education Corporation D/B/A Drexel University College Of Medicine NOVEL P13K p110 INHIBITORS AND METHODS OF USE THEREOF
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
HK1214159A1 (zh) 2012-11-08 2016-07-22 Rhizen Pharmaceuticals S.A. 含有PDE4抑制剂和PI3δ或双重PI3δ-γ激酶抑制剂的药物组合物
EA201690089A1 (ru) 2013-06-11 2017-04-28 Латвийский Институт Органического Синтеза ТИЕНО[2,3-b]ПИРИДИНЫ КАК МОДУЛЯТОРЫ СОСТОЯНИЯ МНОЖЕСТВЕННОЙ ЛЕКАРСТВЕННОЙ УСТОЙЧИВОСТИ
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
EA201692557A1 (ru) 2014-07-04 2017-05-31 Люпин Лимитед Хинолизиноновые производные в качестве ингибиторов pi3k
BR112017003745A2 (pt) 2014-08-29 2017-12-05 Tes Pharma S R L inibidores de semialdeído descarboxilase de ácido alfa-amino-beta-carboximucônico
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
SG10201912302VA (en) 2015-02-27 2020-02-27 Incyte Corp Salts of pi3k inhibitor and processes for their preparation
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
TWI773657B (zh) 2015-12-18 2022-08-11 美商亞德利克斯公司 作爲非全身tgr5促效劑之經取代之4-苯基吡啶化合物
US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
IL278889B2 (en) 2018-06-01 2025-11-01 Incyte Corp Dosing regimen for the treatment of pi3k related disorders

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PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
DE3020458C2 (de) 1980-05-29 1986-07-31 Herzog, Thomas, Prof. Dr., 3500 Kassel Vorgehängte Fassaden-, Bau- oder Dekorationsplatte
US6043062A (en) 1995-02-17 2000-03-28 The Regents Of The University Of California Constitutively active phosphatidylinositol 3-kinase and uses thereof
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
US5822910A (en) 1997-10-02 1998-10-20 Shewmake; I. W. Fishing line tensioning device
HRP20160350T1 (hr) * 2007-03-23 2016-05-06 Amgen Inc. Heterociklički spojevi i njihove uporabe
MX2009010050A (es) * 2007-03-23 2009-10-12 Amgen Inc Derivados de quinolina o quinoxalina 3-sustituidos y su uso como inhibidores de fosfotidilinositol 3-cinasa (p13k).
CN101801933A (zh) 2007-09-26 2010-08-11 安斯泰来制药株式会社 喹诺酮衍生物
WO2010036380A1 (en) * 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
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Publication number Publication date
CA2803259A1 (en) 2012-01-05
EP2588468A1 (en) 2013-05-08
AU2011271460A1 (en) 2013-01-10
WO2012003262A1 (en) 2012-01-05
MX2012014996A (es) 2013-03-21
ES2472720T3 (es) 2014-07-02
AU2011271460B2 (en) 2014-02-06
US8759371B2 (en) 2014-06-24
US20130085151A1 (en) 2013-04-04
EP2588468B1 (en) 2014-03-26

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