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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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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JP2013507448A (ja
JP2013507448A5 (enExample
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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 Active 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 US7741330B1 (en) 2009-10-12 2009-10-16 Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
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
PCT/US2010/052377 WO2011046964A2 (en) 2009-10-12 2010-10-12 Inhibitors of bruton's tyrosine kinase

Related Child Applications (1)

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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)

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JP2013507448A JP2013507448A (ja) 2013-03-04
JP2013507448A5 JP2013507448A5 (enExample) 2013-11-14
JP5717109B2 true JP5717109B2 (ja) 2015-05-13

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JP2012534294A Active 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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US (4) US7718662B1 (enExample)
EP (2) EP2650294B1 (enExample)
JP (2) JP5717109B2 (enExample)
KR (1) KR20120097376A (enExample)
CN (1) CN102656173B (enExample)
AU (1) AU2010306921C1 (enExample)
BR (1) BR112012008624A2 (enExample)
CA (1) CA2776543A1 (enExample)
CL (1) CL2012000917A1 (enExample)
CO (1) CO6531429A2 (enExample)
CR (1) CR20120244A (enExample)
EA (1) EA021715B1 (enExample)
ES (1) ES2590905T3 (enExample)
IL (1) IL219076A (enExample)
IN (1) IN2012DN03012A (enExample)
MX (1) MX2012004258A (enExample)
NZ (1) NZ599396A (enExample)
PH (1) PH12012500712A1 (enExample)
SG (1) SG10201506776RA (enExample)
WO (1) WO2011046964A2 (enExample)
ZA (1) ZA201202552B (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
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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)
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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US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
US20100101977A1 (en) * 2008-06-05 2010-04-29 United Comb & Novelty Corporation Stackable Packaging For Lipped Containers
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
CA3031835C (en) 2008-06-27 2021-09-07 Celgene Car Llc Heteroaryl compounds and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
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PH12012500712A1 (en) 2017-07-26
EP2393816A2 (en) 2011-12-14
AU2010306921C1 (en) 2016-03-17
AU2010306921A1 (en) 2012-05-10
EP2650294B1 (en) 2016-07-20
CO6531429A2 (es) 2012-09-28
EA021715B1 (ru) 2015-08-31
BR112012008624A2 (pt) 2017-06-13
CN102656173A (zh) 2012-09-05
JP2013507448A (ja) 2013-03-04
NZ599396A (en) 2014-03-28
US9012463B2 (en) 2015-04-21
CN102656173B (zh) 2016-03-16
MX2012004258A (es) 2012-05-29
ES2590905T8 (es) 2020-12-09
KR20120097376A (ko) 2012-09-03
WO2011046964A2 (en) 2011-04-21
US7718662B1 (en) 2010-05-18
US7741330B1 (en) 2010-06-22
IL219076A (en) 2016-06-30
EP2650294A1 (en) 2013-10-16
CL2012000917A1 (es) 2012-07-13
US20110086866A1 (en) 2011-04-14
ZA201202552B (en) 2013-11-27
US20140080844A1 (en) 2014-03-20
AU2010306921B2 (en) 2015-08-13
EP2393816A4 (en) 2011-12-14
SG10201506776RA (en) 2015-10-29

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