JP5717109B2 - ブルトン型チロシンキナーゼの阻害剤 - Google Patents

ブルトン型チロシンキナーゼの阻害剤 Download PDF

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Publication number
JP5717109B2
JP5717109B2 JP2012534294A JP2012534294A JP5717109B2 JP 5717109 B2 JP5717109 B2 JP 5717109B2 JP 2012534294 A JP2012534294 A JP 2012534294A JP 2012534294 A JP2012534294 A JP 2012534294A JP 5717109 B2 JP5717109 B2 JP 5717109B2
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formula
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acid
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JP2013507448A (ja
JP2013507448A5 (OSRAM
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チェン・ウェイ
デイビッド・ジェイ・ルーリー
タラク・ディ・モディ
エリック・バーナー
マーク・スティーブン・スマイス
ウェンチェン・ルオ
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Pharmacyclics LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
JP2012534294A 2009-10-12 2010-10-12 ブルトン型チロシンキナーゼの阻害剤 Expired - Fee Related JP5717109B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US25078709P 2009-10-12 2009-10-12
US61/250,787 2009-10-12
US12/581,062 2009-10-16
US12/581,044 US7718662B1 (en) 2009-10-12 2009-10-16 Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
US12/581,044 2009-10-16
US12/581,062 US7741330B1 (en) 2009-10-12 2009-10-16 Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
PCT/US2010/052377 WO2011046964A2 (en) 2009-10-12 2010-10-12 Inhibitors of bruton's tyrosine kinase

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2015047643A Division JP2015134802A (ja) 2009-10-12 2015-03-10 ブルトン型チロシンキナーゼの阻害剤

Publications (3)

Publication Number Publication Date
JP2013507448A JP2013507448A (ja) 2013-03-04
JP2013507448A5 JP2013507448A5 (OSRAM) 2013-11-14
JP5717109B2 true JP5717109B2 (ja) 2015-05-13

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JP2012534294A Expired - Fee Related JP5717109B2 (ja) 2009-10-12 2010-10-12 ブルトン型チロシンキナーゼの阻害剤
JP2015047643A Pending JP2015134802A (ja) 2009-10-12 2015-03-10 ブルトン型チロシンキナーゼの阻害剤

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JP2015047643A Pending JP2015134802A (ja) 2009-10-12 2015-03-10 ブルトン型チロシンキナーゼの阻害剤

Country Status (21)

Country Link
US (4) US7718662B1 (OSRAM)
EP (2) EP2393816A4 (OSRAM)
JP (2) JP5717109B2 (OSRAM)
KR (1) KR20120097376A (OSRAM)
CN (1) CN102656173B (OSRAM)
AU (1) AU2010306921C1 (OSRAM)
BR (1) BR112012008624A2 (OSRAM)
CA (1) CA2776543A1 (OSRAM)
CL (1) CL2012000917A1 (OSRAM)
CO (1) CO6531429A2 (OSRAM)
CR (1) CR20120244A (OSRAM)
EA (1) EA021715B1 (OSRAM)
ES (1) ES2590905T3 (OSRAM)
IL (1) IL219076A (OSRAM)
IN (1) IN2012DN03012A (OSRAM)
MX (1) MX2012004258A (OSRAM)
NZ (1) NZ599396A (OSRAM)
PH (1) PH12012500712A1 (OSRAM)
SG (1) SG10201506776RA (OSRAM)
WO (1) WO2011046964A2 (OSRAM)
ZA (1) ZA201202552B (OSRAM)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015134802A (ja) * 2009-10-12 2015-07-27 ファーマサイクリクス，インコーポレイテッド ブルトン型チロシンキナーゼの阻害剤
US9814721B2 (en) 2010-06-03 2017-11-14 Pharmacyclics Llc Use of inhibitors of bruton'S tyrosine kinase (BTK)
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations
US10954567B2 (en) 2012-07-24 2021-03-23 Pharmacyclics Llc Mutations associated with resistance to inhibitors of Bruton's Tyrosine Kinase (BTK)

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DK2529622T3 (en) 2006-09-22 2018-05-07 Pharmacyclics Llc INHIBITORS OF BRUTON-TYROSINKINASE
US20120101114A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US20090301928A1 (en) * 2008-06-05 2009-12-10 United Comb & Novelty Corporation Packaging For Lipped Containers
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
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US20110224235A1 (en) 2008-07-16 2011-09-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
JP5918693B2 (ja) 2009-05-05 2016-05-18 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 Ｅｇｆｒ阻害剤及び疾患の治療方法
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JP6118794B2 (ja) 2011-04-01 2017-04-19 ザ ユニバーシティ オブ ユタ リサーチ ファウンデイション Ａｘｌキナーゼの阻害剤としての置換ｎ−フェニルピリミジン−２−アミン類似体
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JP6105578B2 (ja) 2011-07-21 2017-03-29 トレロ ファーマシューティカルズ， インコーポレイテッド 複素環式プロテインキナーゼ阻害剤
JP2014532658A (ja) 2011-10-28 2014-12-08 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ブルトン型チロシンキナーゼ疾患または障害を治療する方法
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US7718662B1 (en) * 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
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JP2015134802A (ja) * 2009-10-12 2015-07-27 ファーマサイクリクス，インコーポレイテッド ブルトン型チロシンキナーゼの阻害剤
US9814721B2 (en) 2010-06-03 2017-11-14 Pharmacyclics Llc Use of inhibitors of bruton'S tyrosine kinase (BTK)
US10004746B2 (en) 2010-06-03 2018-06-26 Pharmacyclics Llc Use of inhibitors of Bruton's tyrosine kinase (Btk)
US10004745B2 (en) 2010-06-03 2018-06-26 Pharmacyclics Llc Use of inhibitors of Bruton'S tyrosine kinase (Btk)
US10016435B2 (en) 2010-06-03 2018-07-10 Pharmacyclics Llc Use of inhibitors of Bruton's tyrosine kinase (Btk)
US10478439B2 (en) 2010-06-03 2019-11-19 Pharmacyclics Llc Use of inhibitors of bruton's tyrosine kinase (Btk)
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NZ599396A (en) 2014-03-28
EP2393816A2 (en) 2011-12-14
EA201270553A1 (ru) 2012-09-28
ZA201202552B (en) 2013-11-27
CA2776543A1 (en) 2011-04-21
AU2010306921A1 (en) 2012-05-10
IL219076A (en) 2016-06-30
WO2011046964A2 (en) 2011-04-21
BR112012008624A2 (pt) 2017-06-13
US9012463B2 (en) 2015-04-21
CN102656173A (zh) 2012-09-05
KR20120097376A (ko) 2012-09-03
JP2013507448A (ja) 2013-03-04
US7741330B1 (en) 2010-06-22
ES2590905T8 (es) 2020-12-09
CN102656173B (zh) 2016-03-16
EP2650294B1 (en) 2016-07-20
EA021715B1 (ru) 2015-08-31
CO6531429A2 (es) 2012-09-28
IL219076A0 (en) 2012-06-28
ES2590905T3 (es) 2016-11-24
US20140080844A1 (en) 2014-03-20
SG10201506776RA (en) 2015-10-29
MX2012004258A (es) 2012-05-29
US7718662B1 (en) 2010-05-18
EP2393816A4 (en) 2011-12-14
EP2650294A1 (en) 2013-10-16
WO2011046964A3 (en) 2011-08-25
CR20120244A (es) 2013-01-03
PH12012500712A1 (en) 2017-07-26
AU2010306921C1 (en) 2016-03-17
IN2012DN03012A (OSRAM) 2015-07-31

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