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AR097862A1 - Inhibidores de tirosina quinasa de bruton - Google Patents

Inhibidores de tirosina quinasa de bruton

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Publication number
AR097862A1
AR097862A1 ARP140103633A ARP140103633A AR097862A1 AR 097862 A1 AR097862 A1 AR 097862A1 AR P140103633 A ARP140103633 A AR P140103633A AR P140103633 A ARP140103633 A AR P140103633A AR 097862 A1 AR097862 A1 AR 097862A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
alkyl
heteroalkyl
pharmaceutically acceptable
Prior art date
Application number
ARP140103633A
Other languages
English (en)
Inventor
Chen Wei
Wang Longcheng
J Jia Zhaozhong
J Loury David
Original Assignee
Pharmacyclics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pharmacyclics Inc filed Critical Pharmacyclics Inc
Publication of AR097862A1 publication Critical patent/AR097862A1/es

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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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • 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
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    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • 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
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    • 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
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    • 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
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    • A61P37/02—Immunomodulators
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    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
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  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compuestos que forman enlaces covalentes con la tirosina quinasa de Bruton (Btk). También se describen inhibidores irreversibles de Btk, inhibidores reversibles de Btk y composiciones farmacéuticas que incluyen los compuestos. Además se describen métodos para utilizar los inhibidores Btk, solos o en combinación con otros agentes terapéuticos, para el tratamiento de enfermedades o condiciones autoinmunes, enfermedades o condiciones heteroinmunes, cáncer, incluido el linfoma, y enfermedades o condiciones infamatorias. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque tiene la estructura de fórmula (1), donde: L¹ es -N(R²)C(O)- o -C(O)N(R²)-; R¹ es C₆₋₁₂ arilo o C₃₋₁₂ heteroarilo, donde C₆₋₁₂ arilo y C₃₋₁₂ heteroarilo están opcionalmente sustituidos con al menos un R³; R² es H o C₁₋₄ alquilo; R³ es halógeno, -CF₃, -CN, -NO₂, -OR⁶, -N(R⁶)(R⁷), C₁₋₆ alquilo sustituido o no sustituido, C₃₋₆ cicloalquilo sustituido o no sustituido, o C₁₋₆ heteroalquilo sustituido o no sustituido; R⁴ es H, C₁₋₆ alquilo sustituido o no sustituido, C₁₋₆ heteroalquilo sustituido o no sustituido, C₃₋₈ cicloalquilo sustituido o no sustituido, o C₂₋₉ heterocicloalquilo sustituido o no sustituido; R⁵ es C₃₋₈ cicloalquilo sustituido o no sustituido, o C₂₋₉ heterocicloalquilo sustituido o no sustituido; o R⁴ y R⁵ junto con el átomo de nitrógeno al cual están unidos forman un C₂₋₉ heterocicloalquilo; R⁶ es H, C₁₋₆ alquilo sustituido o no sustituido, o C₁₋₆ heteroalquilo sustituido o no sustituido; R⁷ es H, C₁₋₆ alquilo sustituido o no sustituido, C₁₋₆ heteroalquilo sustituido o no sustituido; R¹⁰ es halógeno, C₁₋₆ alquilo sustituido o no sustituido, o C₁₋₆ alcoxi sustituido o no sustituido; m es 1 ó 2; n es 0 ó 1; y p es 0, 1, ó 2; o una sal farmacéuticamente aceptable, solvato farmacéuticamente aceptable, o prodroga farmacéuticamente aceptable del mismo.
ARP140103633A 2013-09-30 2014-09-30 Inhibidores de tirosina quinasa de bruton AR097862A1 (es)

Applications Claiming Priority (1)

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US201361884888P 2013-09-30 2013-09-30

Publications (1)

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AR097862A1 true AR097862A1 (es) 2016-04-20

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ARP140103633A AR097862A1 (es) 2013-09-30 2014-09-30 Inhibidores de tirosina quinasa de bruton

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US (2) US9624224B2 (es)
EP (1) EP3052486A1 (es)
JP (1) JP2016531941A (es)
KR (1) KR20160062103A (es)
CN (1) CN105764896A (es)
AR (1) AR097862A1 (es)
AU (1) AU2014324532A1 (es)
BR (1) BR112016006978A2 (es)
CA (1) CA2925124A1 (es)
CR (1) CR20160203A (es)
DO (1) DOP2016000071A (es)
EA (1) EA201690618A1 (es)
IL (1) IL244492A0 (es)
MA (1) MA38961A1 (es)
PE (1) PE20160560A1 (es)
PH (1) PH12016500575A1 (es)
SG (1) SG11201602421VA (es)
TN (1) TN2016000094A1 (es)
TW (1) TW201546061A (es)
WO (1) WO2015048689A1 (es)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120087915A1 (en) 2010-06-03 2012-04-12 Pharmacyclics, Inc. Use of inhibitors of bruton's tyrosine kinase (btk)
CA2841080A1 (en) 2011-07-13 2013-01-17 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
PT3409278T (pt) 2011-07-21 2020-12-18 Sumitomo Dainippon Pharma Oncology Inc Inibidores de proteína cinase heterocíclicos
MX2015001081A (es) 2012-07-24 2015-10-14 Pharmacyclics Inc Mutaciones asociadas a resistencia a inhibidores de la tirosina cinasa de bruton (btk).
US10202356B2 (en) 2013-03-14 2019-02-12 Tolero Pharmaceuticals, Inc. JAK2 and ALK2 inhibitors and methods for their use
WO2015002894A1 (en) 2013-07-02 2015-01-08 Pharmacyclics, Inc. Purinone compounds as kinase inhibitors
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations
CN107021963A (zh) * 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
CN108602834B (zh) * 2016-02-05 2021-01-08 北京盛诺基医药科技股份有限公司 一种布鲁顿酪氨酸激酶抑制剂
MX2019006288A (es) 2016-12-03 2020-10-01 Juno Therapeutics Inc Metodos y composiciones para el uso de celulas t terapeuticas en combinacion con inhibidores de quinasa.
KR101956815B1 (ko) 2017-02-14 2019-03-12 한국화학연구원 트리아졸로피리다진 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 브루톤티로신 키나제 활성 관련 질환의 예방 또는 치료용 약학적 조성물
US10314844B2 (en) 2017-02-24 2019-06-11 Gilead Sciences, Inc. Inhibitors of Bruton's tyrosine kinase
CN110312720A (zh) 2017-02-24 2019-10-08 吉利德科学公司 布鲁顿氏酪氨酸激酶的抑制剂
CN108570036A (zh) * 2017-03-09 2018-09-25 北京赛林泰医药技术有限公司 一种btk抑制剂的多晶型物及其制备方法
WO2018208132A1 (en) * 2017-05-12 2018-11-15 Korea Research Institute Of Chemical Technology Pyrazolopyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer, autoimmune disease and brain disease containing the same as an active ingredient
KR102128018B1 (ko) 2017-05-12 2020-06-30 한국화학연구원 피라졸로 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암, 자가면역질환 및 뇌질환의 예방 또는 치료용 약학적 조성물
KR102032418B1 (ko) 2017-06-15 2019-10-16 한국화학연구원 접합 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 브루톤티로신 키나제 활성 관련 질환의 예방 또는 치료용 약학적 조성물
US11161851B2 (en) 2017-11-06 2021-11-02 Suzhou Pengxu Pharmatech Co. Ltd. Processes to produce acalabrutinib
CN109748929A (zh) * 2017-11-06 2019-05-14 苏州鹏旭医药科技有限公司 一种化合物的制备方法
JP2021524835A (ja) 2018-04-05 2021-09-16 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド Ａｘｌキナーゼ阻害剤およびその使用
MX2020010556A (es) 2018-04-13 2021-03-02 Sumitomo Pharma Oncology Inc Inhibidores de cinasa de insercion proviral en linfomas murinos (pim) para el tratamiento de neoplasias mieloproliferativas y fibrosis asociadas con cancer.
JP2021530554A (ja) 2018-07-26 2021-11-11 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド 異常なａｃｖｒ１発現を伴う疾患を処置するための方法およびそこで使用するためのａｃｖｒ１阻害剤
CN110964016B (zh) * 2018-09-29 2021-05-28 南京药捷安康生物科技有限公司 氨基降茨烷衍生物及其制备方法与应用
CA3127502A1 (en) 2019-02-12 2020-08-20 Sumitomo Dainippon Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
WO2020252397A1 (en) * 2019-06-12 2020-12-17 Baylor College Of Medicine Small molecule proteolysis-targeting chimeras and methods of use thereof
CN111018865B (zh) * 2019-10-17 2021-01-15 山东大学 1-取代苄基吡唑并嘧啶衍生物及其制备方法与应用
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN112961159B (zh) * 2020-03-05 2022-07-01 四川大学华西医院 氨基嘧啶并吡唑/吡咯类衍生物及其制备方法和用途
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
CA3223447A1 (en) 2021-06-25 2022-12-29 Korea Research Institute Of Chemical Technology Novel bifunctional heterocyclic compound having btk degradation function via ubiquitin proteasome pathway, and use thereof
KR102637915B1 (ko) 2021-06-25 2024-02-19 한국화학연구원 유비퀴틴 프로테오좀 경로를 통해 비티케이 분해작용을 가지는 신규한 이작용성 헤테로사이클릭 화합물과 이의 용도
WO2023050007A1 (en) * 2021-09-29 2023-04-06 Repare Therapeutics Inc. N-(5-substituted-[(1,3,4-thiadiazolyl) or (thiazolyl)])(substituted)carboxamide compounds and use thereof for inhibiting human polymerase theta
CN114213416B (zh) * 2021-11-05 2023-06-06 杭州医学院 一种恶唑并[4,5-b]吡啶结构的不可逆BTK抑制剂及其应用
CA3237119A1 (en) 2021-11-05 2023-05-11 Song Hee Lee Compound having btk protein degradation activity, and medical uses thereof
CN113968860B (zh) * 2021-11-05 2023-06-06 杭州医学院 一种可逆btk抑制剂及其合成方法和应用
AU2023352129A1 (en) * 2022-09-29 2025-05-01 Repare Therapeutics Inc. N-(5-substituted-[(1,3,4-thiadiazolyl) or (1,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use
CN120302975A (zh) 2022-10-31 2025-07-11 住友制药美国公司 治疗骨髓增生性肿瘤的pim1抑制剂

Family Cites Families (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01167840A (ja) 1987-12-24 1989-07-03 Konica Corp 新規な写真用シアンカプラー
GB9226855D0 (en) 1992-12-23 1993-02-17 Erba Carlo Spa Vinylene-azaindole derivatives and process for their preparation
US6326469B1 (en) 1994-04-22 2001-12-04 Sugen, Inc. Megakaryocytic protein tyrosine kinases
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
ID24653A (id) 1997-03-19 2000-07-27 Basf Ag Zat-zat terapi
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
DE69918089T2 (de) 1998-04-17 2005-07-14 Parker Hughes Institute, St. Paul Btk inhibitoren und verfahren zur identifizierung und verwendung
US6335155B1 (en) 1998-06-26 2002-01-01 Sunesis Pharmaceuticals, Inc. Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
US6998233B2 (en) 1998-06-26 2006-02-14 Sunesis Pharmaceuticals, Inc. Methods for ligand discovery
US20050287596A9 (en) 1998-06-26 2005-12-29 Braisted Andrew C Novel ligands and libraries of ligands
CA2344249A1 (en) 1998-09-18 2000-03-30 Basf Aktiengesellschaft Pyrrolopyrimidines as protein kinase inhibitors
US6713474B2 (en) 1998-09-18 2004-03-30 Abbott Gmbh & Co. Kg Pyrrolopyrimidines as therapeutic agents
US6306897B1 (en) 1999-03-19 2001-10-23 Parker Hughes Institute Calanolides for inhibiting BTK
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
US6660744B1 (en) 1999-09-17 2003-12-09 Abbott Gmbh & Co. Kg Pyrazolopyrimidines as therapeutic agents
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
CA2384378C (en) 1999-10-06 2011-05-24 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
JP2003516351A (ja) 1999-11-30 2003-05-13 パーカー ヒューズ インスティテュート コラーゲン誘導血小板凝集阻害剤
IL150059A0 (en) 1999-12-17 2002-12-01 Ariad Pharma Inc Novel heterocycles
GB0005345D0 (en) 2000-03-06 2000-04-26 Mathilda & Terence Kennedy Ins Methods of treating sepsis septic shock and inflammation
AU2000240570A1 (en) 2000-03-29 2001-10-08 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
EP1373554A2 (en) 2000-10-23 2004-01-02 Bristol-Myers Squibb Company Modulators of bruton's tyronsine kinase, their identification and use
EP1345592A2 (en) 2000-12-06 2003-09-24 Pharmacia Corporation Rapidly dispersing pharmaceutical composition comprising effervescent agents
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
US8306897B2 (en) 2001-05-04 2012-11-06 Stockshield, Inc. Method and system for insuring against investment loss
US20030114467A1 (en) 2001-06-21 2003-06-19 Shakespeare William C. Novel pyrazolo- and pyrrolo-pyrimidines and uses thereof
CA2450777C (en) 2001-08-10 2013-04-09 Novartis Ag Use of c-src inhibitors alone or in combination with sti571 for the treatment of leukaemia
WO2003016338A1 (en) 2001-08-15 2003-02-27 Parker Hughes Institute Crystal structure of the btk kinase domain
AU2002254725A1 (en) 2001-11-21 2003-06-10 Sunesis Pharmaceuticals, Inc. Methods for ligand discovery
US20050084905A1 (en) 2002-03-21 2005-04-21 Prescott John C. Identification of kinase inhibitors
GB2388594A (en) 2002-05-16 2003-11-19 Bayer Ag Imidazo-triazine PDE 4 inhibitors
JP2005536533A (ja) 2002-08-08 2005-12-02 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 置換ベンゾイミダゾール化合物
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US7687506B2 (en) 2003-04-11 2010-03-30 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
WO2004100868A2 (en) 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
EP1473039A1 (en) 2003-05-02 2004-11-03 Centre National De La Recherche Scientifique (Cnrs) Use of inhibitors and antisense oligonucleotides of BTK for the treatment of proliferative mastocytosis
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
WO2005037836A2 (en) 2003-10-15 2005-04-28 Osi Pharmaceuticals, Inc. Imidazo ‘1, 5 - a ! pyrazine tyrosine kinase inhibitors
WO2005060956A1 (en) 2003-12-12 2005-07-07 University Of Maryland, Baltimore IMMUNOMODULATORY COMPOUNDS THAT TARGET AND INHIBIT THE pY+3 BINDING SITE OF TYROSENE KINASE p56 LCK SH2 DOMAIN
BRPI0418031A (pt) 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
CN1934113B (zh) 2004-01-26 2011-11-09 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的组合物
WO2005074603A2 (en) 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
ITMI20041314A1 (it) 2004-06-30 2004-09-30 Nuvera Fuel Cells Europ Srl Dispositivo di raffreddamento per celle a combustibili a membrana
AR053090A1 (es) 2004-07-20 2007-04-25 Osi Pharm Inc Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos
JP2008514635A (ja) 2004-09-27 2008-05-08 コーザン バイオサイエンシス インコーポレイテッド 特異的キナーゼ阻害剤
EP1802602A1 (en) 2004-09-28 2007-07-04 Janssen Pharmaceutica N.V. Substituted dipiperdine ccr2 antagonists
WO2006053121A2 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
KR100735639B1 (ko) 2004-12-29 2007-07-04 한미약품 주식회사 암세포 성장 억제 효과를 갖는 퀴나졸린 유도체 및 이의제조방법
AU2006223409B2 (en) 2005-03-10 2011-07-21 Gilead Connecticut, Inc. Certain substituted amides, method of making, and method of use thereof
CN101175753B (zh) 2005-05-13 2011-03-23 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
MY153898A (en) 2005-06-22 2015-04-15 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
JP2009515879A (ja) 2005-11-12 2009-04-16 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｔｅｃキナーゼ阻害剤
US7625880B2 (en) 2006-01-13 2009-12-01 Pharmacyclics, Inc. Inhibitors of tyrosine kinases and uses thereof
EP2865381A1 (en) 2006-05-18 2015-04-29 Pharmacyclics, Inc. ITK inhibitors for treating blood cell malignancies
EA018573B1 (ru) 2006-09-22 2013-09-30 Фармасайкликс, Инк. Ингибиторы тирозинкиназы брутона
EP2089391B1 (en) 2006-11-03 2013-01-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
NL2000640C2 (nl) 2007-03-05 2008-09-08 Stichting Wetsus Ct Of Excelle Werkwijze en systeem voor het zuiveren van een vloeistof.
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
SG10201508035TA (en) 2007-03-28 2015-10-29 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
US8426441B2 (en) 2007-12-14 2013-04-23 Roche Palo Alto Llc Inhibitors of bruton's tyrosine kinase
US20150152115A1 (en) 2007-12-27 2015-06-04 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
JP5369183B2 (ja) 2008-07-16 2013-12-18 ファーマサイクリックス，インク． 固形腫瘍の治療用のブルートンのチロシンキナーゼの阻害剤
RU2014150660A (ru) 2008-09-05 2015-07-20 Селджен Авиломикс Рисерч, Инк. Алгоритм разработки необратимо действующих ингибиторов
US8426428B2 (en) 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
PL2473049T3 (pl) * 2009-09-04 2019-07-31 Biogen Ma Inc. Inhibitory kinazy tyrozynowej brutona
US20110230476A1 (en) 2009-09-09 2011-09-22 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
ES2592152T3 (es) 2010-05-31 2016-11-28 Ono Pharmaceutical Co., Ltd. Derivado de purinona como inhibidor de Btk quinasa
US20120087915A1 (en) 2010-06-03 2012-04-12 Pharmacyclics, Inc. Use of inhibitors of bruton's tyrosine kinase (btk)
MX342164B (es) 2010-06-23 2016-09-19 Hanmi Science Co Ltd Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa.
US9580427B2 (en) 2011-05-17 2017-02-28 The Regents Of The University Of California Kinase inhibitors
US9376438B2 (en) * 2011-05-17 2016-06-28 Principia Biopharma, Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
KR102027598B1 (ko) 2011-05-17 2019-10-01 프린시피아 바이오파마, 인코퍼레이티드 타이로신 키나아제 저해제
WO2013003629A2 (en) 2011-06-28 2013-01-03 Pharmacyclics, Inc. Methods and compositions for inhibition of bone resorption
CA2841080A1 (en) 2011-07-13 2013-01-17 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
US8501724B1 (en) 2012-01-31 2013-08-06 Pharmacyclics, Inc. Purinone compounds as kinase inhibitors
MX348290B (es) 2012-06-04 2017-06-05 Pharmacyclics Llc Formas cristalinas de un inhibidor de tirosina quinasa de bruton.
WO2013191965A1 (en) 2012-06-18 2013-12-27 Principia Biopharma Inc. Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases
EP2878601B1 (en) 2012-07-27 2018-03-28 Riken Agent for treating or controlling recurrence of acute myelogenous leukemia
WO2014022569A1 (en) 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
MA38183A1 (fr) 2012-11-15 2017-03-31 Pharmacyclics Inc Composés pyrrolopyrimidines en tant qu'inhibiteurs de kinase
US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2015017812A1 (en) 2013-08-02 2015-02-05 Pharmacyclics, Inc. Methods for the treatment of solid tumors
WO2015061752A1 (en) 2013-10-25 2015-04-30 Pharmacyclics, Inc. Treatment using bruton's tyrosine kinase inhibitors and immunotherapy
CN105949198A (zh) 2014-01-29 2016-09-21 苏州晶云药物科技有限公司 依鲁替尼的新晶型及其制备方法
WO2015127261A1 (en) 2014-02-21 2015-08-27 Pharmacyclics, Inc. Biomarkers for predicting response of dlbcl to treatment with ibrutinib
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations

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