[go: up one dir, main page]

EA201690618A1 - Ингибиторы тирозинкиназы брутона - Google Patents

Ингибиторы тирозинкиназы брутона

Info

Publication number
EA201690618A1
EA201690618A1 EA201690618A EA201690618A EA201690618A1 EA 201690618 A1 EA201690618 A1 EA 201690618A1 EA 201690618 A EA201690618 A EA 201690618A EA 201690618 A EA201690618 A EA 201690618A EA 201690618 A1 EA201690618 A1 EA 201690618A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
btk
conditions
compounds
bluton
Prior art date
Application number
EA201690618A
Other languages
English (en)
Inventor
Лунчэн Ван
Вэй Чэнь
Чжаочжун Дж. Цзя
Дэвид Дж. Лоури
Original Assignee
Фармасайкликс Элэлси
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 Фармасайкликс Элэлси filed Critical Фармасайкликс Элэлси
Publication of EA201690618A1 publication Critical patent/EA201690618A1/ru

Links

Classifications

    • 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
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0031Rectum, anus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078Sprays 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • 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
    • A61P19/00Drugs for skeletal disorders
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • 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)
  • Zoology (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dispersion Chemistry (AREA)
  • Otolaryngology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nutrition Science (AREA)
  • Physiology (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

Описанные в данном документе соединения, представляют собой соединения, которые образуют ковалентные связи с тирозинкиназой Брутона (Btk). Также описанны необратимые ингибиторы Btk. Кроме того, также описаны обратимые ингибиторы Btk. Также описанны фармацевтические композиции, которые включают соединения. Описаны способы использования ингибиторов Btk, отдельно или в комбинации с другими лекарственными средствами, для лечения аутоиммунных заболеваний или состояний, гетероиммунных заболеваний или состояний, рака, включая лимфому, и воспалительных заболеваний или состояний.
EA201690618A 2013-09-30 2014-09-29 Ингибиторы тирозинкиназы брутона EA201690618A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361884888P 2013-09-30 2013-09-30
PCT/US2014/058132 WO2015048689A1 (en) 2013-09-30 2014-09-29 Inhibitors of bruton's tyrosine kinase

Publications (1)

Publication Number Publication Date
EA201690618A1 true EA201690618A1 (ru) 2016-09-30

Family

ID=52740746

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690618A EA201690618A1 (ru) 2013-09-30 2014-09-29 Ингибиторы тирозинкиназы брутона

Country Status (20)

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

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5841998B2 (ja) 2010-06-03 2016-01-13 ファーマサイクリックス,インク. ブルトン型チロシンキナーゼ(Btk)の阻害剤の使用
CN103857396A (zh) 2011-07-13 2014-06-11 药品循环公司 布鲁顿酪氨酸激酶抑制剂
EP3409278B8 (en) 2011-07-21 2020-11-04 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
CA2879570A1 (en) 2012-07-24 2014-01-30 Pharmacyclics, Inc. Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
CA2905993C (en) 2013-03-14 2022-12-06 Tolero Pharmaceuticals, Inc. Substituted 4-amino-pyrimidinyl-2-amino-phenyl derivatives and pharmaceutical compositions thereof for use as jak2 and alk2 inhibitors
EP3016953A4 (en) 2013-07-02 2017-03-01 Pharmacyclics, LLC Purinone compounds as kinase inhibitors
EP3119910A4 (en) 2014-03-20 2018-02-21 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
CN110545826A (zh) 2016-12-03 2019-12-06 朱诺治疗学股份有限公司 用于与激酶抑制剂组合使用治疗性t细胞的方法和组合物
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
AU2018224136B2 (en) 2017-02-24 2021-10-21 Gilead Sciences, Inc. Inhibitors of Bruton's Tyrosine Kinase
JP2020508326A (ja) 2017-02-24 2020-03-19 ギリアド サイエンシズ, 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
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
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
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
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
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
WO2019090269A1 (en) 2017-11-06 2019-05-09 Peng Wang Processes to produce acalabrutinib
AU2019247498A1 (en) 2018-04-05 2020-11-26 Sumitomo Pharma Oncology, Inc. AXL kinase inhibitors and use of the same
CN117959303A (zh) 2018-04-13 2024-05-03 住友制药肿瘤公司 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂
MX2021000977A (es) 2018-07-26 2021-04-12 Sumitomo Pharma Oncology Inc Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos.
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
KR20210146290A (ko) 2019-02-12 2021-12-03 스미토모 다이니폰 파마 온콜로지, 인크. 헤테로시클릭 단백질 키나제 억제제를 포함하는 제제
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
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
KR102637915B1 (ko) 2021-06-25 2024-02-19 한국화학연구원 유비퀴틴 프로테오좀 경로를 통해 비티케이 분해작용을 가지는 신규한 이작용성 헤테로사이클릭 화합물과 이의 용도
WO2022270994A1 (ko) 2021-06-25 2022-12-29 한국화학연구원 유비퀴틴 프로테오좀 경로를 통해 비티케이 분해작용을 가지는 신규한 이작용성 헤테로사이클릭 화합물과 이의 용도
TW202317086A (zh) * 2021-09-29 2023-05-01 加拿大商修復治療公司 化合物、醫藥組成物及製備化合物之方法及其使用方法
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
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
WO2023080732A1 (ko) 2021-11-05 2023-05-11 주식회사 유빅스테라퓨틱스 Btk 단백질 분해 활성을 갖는 화합물 및 이들의 의약 용도
WO2024069592A1 (en) * 2022-09-29 2024-04-04 Repare Therapeutics Inc. N-(5-substituted-[(l,3,4-thiadiazolyl) or (l,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use
WO2024097653A1 (en) 2022-10-31 2024-05-10 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms

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.
WO1997049706A1 (en) 1996-06-25 1997-12-31 Novartis Ag SUBSTITUTED 7-AMINO-PYRROLO[3,2-d]PYRIMIDINES AND THE USE THEREOF
HUP0001507A3 (en) 1997-03-19 2002-01-28 Abbott Gmbh & Co Kg Pyrrolo [2,3-d] pyrimidine derivatives, process for their preparation, their use and pharmaceutical compositions containing them
IL139080A0 (en) 1998-04-17 2001-11-25 Parker Hughes Inst Btx inhibitors and methods for their indentification and use
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
US20050287596A9 (en) 1998-06-26 2005-12-29 Braisted Andrew C Novel ligands and libraries of ligands
US6998233B2 (en) 1998-06-26 2006-02-14 Sunesis Pharmaceuticals, Inc. Methods for ligand discovery
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
SK3842001A3 (en) 1998-09-18 2002-04-04 Basf Ag Pyrrolopyrimidines as protein kinase inhibitors (revised)
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
ATE247657T1 (de) 1999-09-17 2003-09-15 Basf Ag Pyrazolopyrimidine als arzneimittel
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
ES2225231T3 (es) 1999-10-06 2005-03-16 Boehringer Ingelheim Pharmaceuticals Inc. Compuestos heterociclicos, utiles como inhibidores de tirosina quinasas.
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
EP1235567A2 (en) 1999-11-30 2002-09-04 Parker Hughes Institute Inhibitors of collagen-induced platelet aggregation
CA2394650A1 (en) 1999-12-17 2001-06-21 Chi B. Vu Novel heterocycles
GB0005345D0 (en) 2000-03-06 2000-04-26 Mathilda & Terence Kennedy Ins Methods of treating sepsis septic shock and inflammation
WO2001072751A1 (en) 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
CA2426508A1 (en) 2000-10-23 2002-05-16 Bristol-Myers Squibb Company Modulators of bruton's tyrosine kinase and bruton's tyrosine kinase intermediates and methods for their identification and use in the treatment and prevention of osteoporosis and related disease states
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
AU2002315389A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
EP1418917A1 (en) 2001-08-10 2004-05-19 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
NZ532579A (en) 2001-11-21 2006-11-30 Sunesis Pharmaceuticals Inc Methods for ligand discovery based on tethering process
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
CA2494942A1 (en) 2002-08-08 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted benzimidazole compounds
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
WO2005005429A1 (en) 2003-06-30 2005-01-20 Cellular Genomics, 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
AR046337A1 (es) 2003-10-15 2005-12-07 Osi Pharm Inc Imidazopirazina inhibidoras de las tirosinquinasas
US20070196395A1 (en) 2003-12-12 2007-08-23 Mackerell Alexander Immunomodulatory compounds that target and inhibit the py'binding site of tyrosene kinase p56 lck sh2 domain
US20070281907A1 (en) 2003-12-22 2007-12-06 Watkins William J Kinase Inhibitor Phosphonate Conjugates
EP1716151A1 (en) 2004-01-26 2006-11-02 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
EP1730148A4 (en) 2004-02-03 2009-08-19 Abbott Lab USE OF 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
MY139689A (en) 2004-07-20 2009-10-30 Osi Pharm Inc Imidazotriazines as protein kinase inhibitors
WO2006036941A2 (en) 2004-09-27 2006-04-06 Kosan Biosciences Incorporated Specific kinase inhibitors
CN101065374A (zh) 2004-09-28 2007-10-31 詹森药业有限公司 取代的二哌啶化学引诱物细胞因子受体2拮抗剂
EP1812442A2 (en) 2004-11-10 2007-08-01 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
TW200716551A (en) 2005-03-10 2007-05-01 Cgi Pharmaceuticals Inc Certain substituted amides, method of making, and method of use thereof
AU2006247757B2 (en) 2005-05-13 2009-08-27 Irm, Llc Compounds and compositions as protein kinase inhibitors
HUE027370T2 (en) 2005-06-22 2016-10-28 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
WO2007058832A2 (en) 2005-11-12 2007-05-24 Boehringer Ingelheim International Gmbh Pyrrolo (2, 3-b) pyridine derivatives useful as tec kinase inhibitors
CA2636696A1 (en) 2006-01-13 2007-08-02 Pharmacyclics, Inc. Inhibitors of tyrosine kinases and uses thereof
MX2008014450A (es) 2006-05-18 2009-03-09 Mannkind Corp Inhibidores de cinasa intracelular.
HUE025459T2 (hu) 2006-09-22 2016-05-30 Pharmacyclics Inc A Bruton-féle tirozin-kináz inhibitorai
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.
EP2543375A1 (en) 2007-03-28 2013-01-09 Pharmacyclics, Inc. Pyrrolo-pyrimidine analogues as inhibitors of bruton's tyrosine kinase
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US20120101114A1 (en) 2007-03-28 2012-04-26 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
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
WO2010028236A1 (en) 2008-09-05 2010-03-11 Avila Therapeutics, Inc. Algorithm for designing irreversible inhibitors
US8426428B2 (en) 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
PT2473049T (pt) * 2009-09-04 2019-03-04 Sunesis Pharmaceuticals Inc Inibidores de tirosina quinase de bruton
TW201609747A (zh) 2009-09-09 2016-03-16 阿維拉製藥公司 Pi3激酶抑制劑及其用途
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
AU2011260961B9 (en) 2010-05-31 2015-02-26 Ono Pharmaceutical Co., Ltd. Purinone derivative
JP5841998B2 (ja) 2010-06-03 2016-01-13 ファーマサイクリックス,インク. ブルトン型チロシンキナーゼ(Btk)の阻害剤の使用
NZ605988A (en) 2010-06-23 2014-11-28 Hanmi Science Co Ltd Novel fused pyrimidine derivatives for inhibition of tyrosine kinase activity
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
BR112013029508B1 (pt) 2011-05-17 2022-05-03 Principia Biopharma, Inc. Composto, composição farmacêutica, e, uso do referido composto
MX2014000130A (es) 2011-06-28 2014-05-01 Pharmacyclics Inc Procedimientos y composiciones para la inhibicion de resorcion osea.
CN103857396A (zh) 2011-07-13 2014-06-11 药品循环公司 布鲁顿酪氨酸激酶抑制剂
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
NZ731932A (en) 2012-06-04 2018-09-28 Pharmacyclics Llc Crystalline forms of a bruton’s tyrosine kinase inhibitor
CA2874461C (en) 2012-06-18 2021-10-12 Principia Biopharma Inc. Formulations containing reversible covalent compounds
WO2014017659A1 (ja) 2012-07-27 2014-01-30 独立行政法人理化学研究所 急性骨髄性白血病の治療又は再発抑制剤
WO2014022569A1 (en) 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
MX2015006168A (es) 2012-11-15 2015-08-10 Pharmacyclics Inc Compuestos de pirrolopirimidina como inhibidores de quinasas.
US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
TWI649081B (zh) 2013-08-02 2019-02-01 製藥公司 治療固態腫瘤之方法
AU2014339816B2 (en) 2013-10-25 2020-05-28 Pharmacyclics Llc Treatment using Bruton's tyrosine kinase inhibitors and immunotherapy
CN106008521A (zh) 2014-01-29 2016-10-12 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
US20150238490A1 (en) 2014-02-21 2015-08-27 Pharmacyclics, Inc. Biomarkers for predicting response of dlbcl to treatment with ibrutinib
EP3119910A4 (en) 2014-03-20 2018-02-21 Pharmacyclics LLC Phospholipase c gamma 2 and resistance associated mutations

Also Published As

Publication number Publication date
PH12016500575A1 (en) 2016-07-25
BR112016006978A2 (pt) 2017-08-01
AR097862A1 (es) 2016-04-20
CA2925124A1 (en) 2015-04-02
CN105764896A (zh) 2016-07-13
US9624224B2 (en) 2017-04-18
WO2015048689A8 (en) 2015-05-07
TN2016000094A1 (en) 2017-07-05
JP2016531941A (ja) 2016-10-13
SG11201602421VA (en) 2016-04-28
US20150094319A1 (en) 2015-04-02
PE20160560A1 (es) 2016-06-09
CR20160203A (es) 2016-08-31
AU2014324532A1 (en) 2016-04-21
MA38961A1 (fr) 2018-05-31
WO2015048689A1 (en) 2015-04-02
DOP2016000071A (es) 2016-09-15
EP3052486A1 (en) 2016-08-10
TW201546061A (zh) 2015-12-16
US20170050970A1 (en) 2017-02-23
KR20160062103A (ko) 2016-06-01
IL244492A0 (en) 2016-04-21

Similar Documents

Publication Publication Date Title
EA201690618A1 (ru) Ингибиторы тирозинкиназы брутона
EA201590855A1 (ru) Соединения пирролопиримидина как ингибиторы киназ
MX375752B (es) Inhibidores de tirosina quinasa de bruton.
PH12014501815A1 (en) Purinone compounds as kinase inhibitors
NI201500059A (es) Inhibidores de la tirosina-quinasa de bruton
TW201613919A (en) Inhibitors of Bruton's tyrosine kinase
MX2017015574A (es) Inhibidores de tirosina quinasa de bruton.
EA201691059A1 (ru) Соединения-пептидомиметики и содержащие их конъюгаты антитело-лекарственное средство
EA201591524A1 (ru) Производные 2-аминопиримидина для лечения вирусных инфекций
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA202092456A3 (ru) Комбинированная терапия, включающая ингибитор mdm2 и один или более дополнительных фармацевтически активных агентов, для лечения различных видов рака
CL2015001985A1 (es) Compuestos de tiazolcarboxamidas y piridinacarboxamida, inhibidores de quinasa pim.
EA201691079A1 (ru) Комбинированная терапия для лечения онкологического заболевания
EA202090683A3 (ru) Способы и композиции для лечения рака
EA201690093A1 (ru) Производные пирроло[3,2-d]пиримидина для лечения вирусных инфекций и других заболеваний
EA201691032A1 (ru) Производные изохромена в качестве ингибиторов фосфоинозитид-3-киназ
EA201591925A1 (ru) Терапевтические композиции и их применение
EA201690039A1 (ru) Ингибиторы rorc2 и способы их применения
EA201690783A1 (ru) Вещества, фармацевтическая композиция и методы применения при лечении воспалительных заболеваний
EA201592242A1 (ru) Производные пиридона для лечения вирусных инфекций и других заболеваний
TW201613926A (en) Inhibitors of bruton's tyrosine kinase
EA201592190A1 (ru) ((пиримидин-4-ил)окси)-1h-индол-1-карбоксамидные производные и их применение
UA110910C2 (uk) Карбоксамідні похідні піразолу як інгібітори тирозинкінази брутона, фармацевтична композиція на їх основі та спосіб лікування захворювань (варіанти)
EA202091908A2 (ru) Комбинированная терапия для лечения онкологического заболевания