JP5976828B2 - Btk活性阻害剤としてのアルキル化ピペラジン化合物 - Google Patents

Btk活性阻害剤としてのアルキル化ピペラジン化合物 Download PDF

Info

Publication number
JP5976828B2
JP5976828B2 JP2014541115A JP2014541115A JP5976828B2 JP 5976828 B2 JP5976828 B2 JP 5976828B2 JP 2014541115 A JP2014541115 A JP 2014541115A JP 2014541115 A JP2014541115 A JP 2014541115A JP 5976828 B2 JP5976828 B2 JP 5976828B2
Authority
JP
Japan
Prior art keywords
cancer
mmol
methyl
compound
mixture
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2014541115A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014532763A (ja
Inventor
ジェームズ ジョン クロフォード,
ジェームズ ジョン クロフォード,
ウェンディ ビー. ヤング,
ウェンディ ビー. ヤング,
Original Assignee
エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト
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 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト filed Critical エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト
Publication of JP2014532763A publication Critical patent/JP2014532763A/ja
Application granted granted Critical
Publication of JP5976828B2 publication Critical patent/JP5976828B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-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
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • 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
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2014541115A 2011-11-03 2012-11-02 Btk活性阻害剤としてのアルキル化ピペラジン化合物 Expired - Fee Related JP5976828B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161555395P 2011-11-03 2011-11-03
US61/555,395 2011-11-03
PCT/US2012/063198 WO2013067277A1 (en) 2011-11-03 2012-11-02 Alkylated piperazine compounds as inhibitors of btk activity

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2015165095A Division JP2016028045A (ja) 2011-11-03 2015-08-24 Btk活性阻害剤としてのアルキル化ピペラジン化合物

Publications (2)

Publication Number Publication Date
JP2014532763A JP2014532763A (ja) 2014-12-08
JP5976828B2 true JP5976828B2 (ja) 2016-08-24

Family

ID=47146780

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2014541115A Expired - Fee Related JP5976828B2 (ja) 2011-11-03 2012-11-02 Btk活性阻害剤としてのアルキル化ピペラジン化合物
JP2015165095A Withdrawn JP2016028045A (ja) 2011-11-03 2015-08-24 Btk活性阻害剤としてのアルキル化ピペラジン化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2015165095A Withdrawn JP2016028045A (ja) 2011-11-03 2015-08-24 Btk活性阻害剤としてのアルキル化ピペラジン化合物

Country Status (23)

Country Link
US (3) US8729072B2 (enExample)
EP (1) EP2773639B1 (enExample)
JP (2) JP5976828B2 (enExample)
KR (1) KR101716011B1 (enExample)
CN (1) CN104024255B (enExample)
AR (1) AR088642A1 (enExample)
AU (1) AU2012332368A1 (enExample)
BR (1) BR112014010439A2 (enExample)
CA (1) CA2853970A1 (enExample)
CL (1) CL2014001158A1 (enExample)
CO (1) CO6950475A2 (enExample)
CR (1) CR20140187A (enExample)
EA (1) EA027561B1 (enExample)
IL (1) IL232280A0 (enExample)
IN (1) IN2014CN03265A (enExample)
MA (1) MA35725B1 (enExample)
MX (1) MX2014005289A (enExample)
PE (1) PE20141686A1 (enExample)
PH (1) PH12014500966A1 (enExample)
SG (1) SG11201401993RA (enExample)
TW (1) TW201326171A (enExample)
WO (1) WO2013067277A1 (enExample)
ZA (1) ZA201403158B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016028045A (ja) * 2011-11-03 2016-02-25 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Btk活性阻害剤としてのアルキル化ピペラジン化合物
JP2020183397A (ja) * 2011-11-03 2020-11-12 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Btk活性阻害剤としてのヘテロアリールピリドン及びアザピリドン化合物

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013021374A2 (en) 2011-08-05 2013-02-14 Mitraltech Ltd. Techniques for percutaneous mitral valve replacement and sealing
CN110698481B (zh) 2013-07-03 2023-02-28 豪夫迈·罗氏有限公司 杂芳基吡啶酮和氮杂-吡啶酮酰胺化合物
KR101813830B1 (ko) 2013-12-05 2017-12-29 에프. 호프만-라 로슈 아게 친전자성 작용기를 갖는 헤테로아릴 피리돈 및 아자-피리돈 화합물
US9908872B2 (en) 2013-12-13 2018-03-06 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
AU2014361798B2 (en) 2013-12-13 2020-06-11 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
WO2015151006A1 (en) 2014-03-29 2015-10-08 Lupin Limited Substituted purine compounds as btk inhibitors
WO2015154064A2 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
WO2015170266A1 (en) 2014-05-07 2015-11-12 Lupin Limited Substituted pyrimidine compounds as btk inhibitors
CN111303159A (zh) * 2014-10-02 2020-06-19 豪夫迈·罗氏有限公司 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物
EP3715346B1 (en) 2014-10-22 2024-01-03 Dana-Farber Cancer Institute, Inc. Thiazolyl-containing compounds for treating proliferative diseases
EP3212645B1 (en) 2014-10-27 2018-11-28 F.Hoffmann-La Roche Ag Process for making tricyclic lactam compounds
CN105837576B (zh) 2015-01-14 2019-03-26 湖北生物医药产业技术研究院有限公司 Btk抑制剂
CU24509B1 (es) * 2015-03-10 2021-05-12 Aurigene Discovery Tech Ltd Compuestos de 1,2,4-oxadiazol y tiadiazol como inmunomoduladores
US10246461B2 (en) 2016-02-29 2019-04-02 Genentech, Inc. Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase
MA46995A (fr) 2016-12-03 2019-10-09 Acerta Pharma Bv Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase
IL284690B (en) * 2016-12-15 2022-07-01 Hoffmann La Roche Process for preparing btk inhibitors
CN107445981B (zh) * 2017-08-25 2018-06-22 牡丹江医学院 一种用于防治宫颈炎的活性化合物
EP3930717A1 (en) 2019-02-25 2022-01-05 Guangzhou Lupeng Pharmaceutical Company Ltd. Inhibitor of btk and mutants thereof
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
US20220363689A1 (en) 2019-10-05 2022-11-17 Newave Pharmaceutical Inc. Inhibitor of btk and mutants thereof
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202140488A (zh) 2020-02-20 2021-11-01 大陸商和記黃埔醫藥(上海)有限公司 雜芳基雜環化合物及其用途
US20230158031A1 (en) * 2020-04-22 2023-05-25 Principia Biopharma Inc. Treatment of Acute Respiratory Distress Syndrome and Other Disorders Involving Cytokine Storm Using BTK Inhibitors
WO2021254483A1 (zh) * 2020-06-18 2021-12-23 上海华汇拓医药科技有限公司 布鲁顿酪氨酸激酶抑制剂及其制备方法
CN116568687B (zh) 2020-09-21 2025-09-02 和记黄埔医药(上海)有限公司 杂芳基杂环化合物及其用途
US20230382900A1 (en) 2020-10-30 2023-11-30 Newave Pharmaceutical Inc. Inhibitors of btk
WO2022133184A1 (en) 2020-12-20 2022-06-23 Newave Pharmaceutical Inc. Btk degrader
CN118613470B (zh) * 2022-01-28 2025-08-15 和记黄埔医药(上海)有限公司 7,8-二氢-2h-环戊二烯并吡咯并吡嗪酮化合物的合成方法

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH08336393A (ja) 1995-04-13 1996-12-24 Mitsubishi Chem Corp 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法
US6602677B1 (en) 1997-09-19 2003-08-05 Promega Corporation Thermostable luciferases and methods of production
US8828902B2 (en) 2001-07-12 2014-09-09 Reaxa Limited Microencapsulated catalyst methods of preparation and method of use thereof
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. 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
WO2006053121A2 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
CA2601628C (en) 2005-03-10 2014-05-13 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
EP1934174B1 (en) 2005-10-07 2011-04-06 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
AR063946A1 (es) 2006-09-11 2009-03-04 Cgi Pharmaceuticals Inc Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
US7838523B2 (en) 2006-09-11 2010-11-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
CL2008002793A1 (es) 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
US8426441B2 (en) 2007-12-14 2013-04-23 Roche Palo Alto Llc Inhibitors of bruton's tyrosine kinase
US7683064B2 (en) 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
WO2009137596A1 (en) 2008-05-06 2009-11-12 Cgi Pharmaceuticals, Inc. Substituted amides, method of making, and use as btk inhibitors
NZ601700A (en) 2008-06-24 2013-02-22 Hoffmann La Roche 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives as inhibitors of Bruton's Tyrosine Kinase (Btk)
PL2300459T3 (pl) 2008-07-02 2013-10-31 Hoffmann La Roche Nowe fenylopirazynony jako inhibitory kinazy
EP2307413B1 (en) 2008-07-15 2015-09-09 F. Hoffmann-La Roche AG Novel phenyl-imidazopyridines and pyridazines
WO2010056875A1 (en) 2008-11-12 2010-05-20 Cgi Pharmaceuticals, Inc. Pyridazinones and their use as btk inhibitors
US8299077B2 (en) * 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
SG175287A1 (en) * 2009-04-24 2011-11-28 Hoffmann La Roche Inhibitors of bruton's tyrosine kinase
EP2424368B1 (en) * 2009-04-29 2014-12-31 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
TWI711610B (zh) * 2009-09-04 2020-12-01 美商百健Ma公司 布魯頓氏酪胺酸激酶抑制劑
EP2566869B1 (en) * 2010-05-07 2016-03-02 Gilead Connecticut, Inc. Pyridone and aza-pyridone compounds and methods of use
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
CN106220614B (zh) 2010-09-01 2019-07-16 吉利德康涅狄格有限公司 吡啶酮/吡嗪酮、其制备方法及使用方法
KR101864908B1 (ko) 2010-09-01 2018-06-05 질레드 코네티컷 인코포레이티드 피리다지논, 그의 제조 방법 및 사용 방법
AU2012257802A1 (en) 2011-05-17 2013-10-31 F. Hoffmann-La Roche Ag Inhibitors of Bruton's tyrosine kinase
PE20140865A1 (es) 2011-08-17 2014-07-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
SG11201401993RA (en) * 2011-11-03 2014-05-29 Hoffmann La Roche Alkylated piperazine compounds as inhibitors of btk activity
UA111756C2 (uk) * 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016028045A (ja) * 2011-11-03 2016-02-25 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Btk活性阻害剤としてのアルキル化ピペラジン化合物
JP2020183397A (ja) * 2011-11-03 2020-11-12 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Btk活性阻害剤としてのヘテロアリールピリドン及びアザピリドン化合物

Also Published As

Publication number Publication date
SG11201401993RA (en) 2014-05-29
US20130116245A1 (en) 2013-05-09
WO2013067277A1 (en) 2013-05-10
EA027561B1 (ru) 2017-08-31
CL2014001158A1 (es) 2014-09-12
EA201490859A1 (ru) 2014-09-30
US8946213B2 (en) 2015-02-03
CA2853970A1 (en) 2013-05-10
IL232280A0 (en) 2014-06-30
JP2014532763A (ja) 2014-12-08
CN104024255A (zh) 2014-09-03
JP2016028045A (ja) 2016-02-25
PH12014500966A1 (en) 2014-06-09
AR088642A1 (es) 2014-06-25
CN104024255B (zh) 2017-01-18
AU2012332368A1 (en) 2014-05-22
US20140221365A1 (en) 2014-08-07
MA35725B1 (fr) 2014-12-01
KR20140090227A (ko) 2014-07-16
PE20141686A1 (es) 2014-11-08
EP2773639A1 (en) 2014-09-10
CO6950475A2 (es) 2014-05-20
TW201326171A (zh) 2013-07-01
EP2773639B1 (en) 2017-04-26
US9115152B2 (en) 2015-08-25
US20150094302A1 (en) 2015-04-02
KR101716011B1 (ko) 2017-03-13
CR20140187A (es) 2014-06-20
BR112014010439A2 (pt) 2017-04-18
MX2014005289A (es) 2014-05-30
US8729072B2 (en) 2014-05-20
ZA201403158B (en) 2017-09-27
IN2014CN03265A (enExample) 2015-07-03

Similar Documents

Publication Publication Date Title
JP5976828B2 (ja) Btk活性阻害剤としてのアルキル化ピペラジン化合物
JP6165977B2 (ja) ヘテロアリールピリドン及びアザ−ピリドンアミド化合物
JP5808869B2 (ja) 二環式ピペラジン化合物
JP5842004B2 (ja) ピリダジノン、その製造方法及びその使用方法
US10344040B2 (en) Pyridone and aza-pyridone compounds and methods of use
JP5976826B2 (ja) Btk活性阻害剤としての8−フルオロフタラジン−1(2h)−オン化合物
JP5841602B2 (ja) ピリジノン/ピラジノン、その作製方法、および使用方法
KR101813830B1 (ko) 친전자성 작용기를 갖는 헤테로아릴 피리돈 및 아자-피리돈 화합물
JP6507234B2 (ja) ブルトンチロシンキナーゼ(btk)によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物
HK1197401B (en) Alkylated piperazine compounds as inhibitors of btk activity
HK1197401A (en) Alkylated piperazine compounds as inhibitors of btk activity
HK1201268B (zh) 二环哌嗪化合物

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150224

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150525

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150723

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150824

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160223

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160523

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20160621

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160720

R150 Certificate of patent or registration of utility model

Ref document number: 5976828

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees