CA2841887A1 - 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk - inhibitors - Google Patents

4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk - inhibitors Download PDF

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Publication number
CA2841887A1
CA2841887A1 CA2841887A CA2841887A CA2841887A1 CA 2841887 A1 CA2841887 A1 CA 2841887A1 CA 2841887 A CA2841887 A CA 2841887A CA 2841887 A CA2841887 A CA 2841887A CA 2841887 A1 CA2841887 A1 CA 2841887A1
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CA
Canada
Prior art keywords
benzamide
pyrazin
methylimidazo
alkyl
propylpyridin
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.)
Abandoned
Application number
CA2841887A
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English (en)
French (fr)
Inventor
De Adrianus Petrus Antonius Man
Jacobus C.H.M. Wijkmans
Jan-Gerard Sterrenburg
Hans C.A. Raaijmakers
Tjeerd A. Barf
Rogier Christian Buijsman
Arthur A. Oubrie
Johannes Bernardus Maria Rewinkel
Christiaan Gerardus Johannes Maria Jans
Herman Thijs Stock
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme BV
Original Assignee
Merck Sharp & Dohme BV
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 Merck Sharp & Dohme BV filed Critical Merck Sharp & Dohme BV
Publication of CA2841887A1 publication Critical patent/CA2841887A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2841887A 2011-07-19 2012-07-11 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk - inhibitors Abandoned CA2841887A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161509376P 2011-07-19 2011-07-19
EP11174582.4 2011-07-19
EP11174582 2011-07-19
US61/509,376 2011-07-19
PCT/EP2012/063556 WO2013010869A1 (en) 2011-07-19 2012-07-11 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides btk-inhibitors

Publications (1)

Publication Number Publication Date
CA2841887A1 true CA2841887A1 (en) 2013-01-24

Family

ID=47557678

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2841887A Abandoned CA2841887A1 (en) 2011-07-19 2012-07-11 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk - inhibitors

Country Status (6)

Country Link
US (1) US20140155406A1 (enExample)
EP (1) EP2734523A1 (enExample)
JP (1) JP2014522860A (enExample)
AU (1) AU2012285988B2 (enExample)
CA (1) CA2841887A1 (enExample)
WO (1) WO2013010869A1 (enExample)

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EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
HK1206073A1 (en) 2012-07-24 2015-12-31 药品循环有限责任公司 Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
SMT201900344T1 (it) 2012-09-10 2019-07-11 Principia Biopharma Inc Composti di pirazolopirimidina come inibitori di chinasi
JP6313772B2 (ja) * 2012-10-04 2018-04-18 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション チロシン受容体キナーゼｂｔｋ阻害剤である置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体
WO2014113942A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
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US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
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US9834554B2 (en) 2013-12-20 2017-12-05 Merck Sharp & Dohme Corp. BTK inhibitors
US9637486B2 (en) 2013-12-20 2017-05-02 Merck Sharp & Dohme Corp. Btk inhibitors
US10272083B2 (en) 2014-01-21 2019-04-30 Acerta Pharma B.V. Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor
CN112353806A (zh) 2014-02-21 2021-02-12 普林斯匹亚生物制药公司 Btk抑制剂的盐和固体形式
CN106456642A (zh) 2014-03-12 2017-02-22 诺华股份有限公司 含btk抑制剂与akt抑制剂的组合
WO2015185998A2 (en) 2014-04-11 2015-12-10 Acerta Pharma B.V. Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase
US9937171B2 (en) 2014-04-11 2018-04-10 Acerta Pharma B.V. Methods of blocking the CXCR-4/SDF-1 signaling pathway with inhibitors of bruton's tyrosine kinase
WO2015193740A2 (en) 2014-06-17 2015-12-23 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor and/or a jak-2 inhibitor
WO2016020901A1 (en) 2014-08-07 2016-02-11 Acerta Pharma B.V. Methods of treating cancers, immune and autoimmune diseases, and inflammatory diseases based on btk occupancy and btk resynthesis rate
US20170231995A1 (en) 2014-08-11 2017-08-17 Acerta Pharma B.V. BTK Inhibitors to Treat Solid Tumors Through Modulation of the Tumor Microenvironment
WO2016024232A1 (en) 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
RS63364B1 (sr) 2014-08-11 2022-07-29 Acerta Pharma Bv Terapeutske kombinacije btk inhibitora, pd-1 inhibitora i/ili pd-l1 inhibitora
SMT202100674T1 (it) 2014-08-11 2022-01-10 Acerta Pharma Bv Combinazioni terapeutiche di un inibitore di btk e un inibitore di bcl-2
WO2016087994A1 (en) 2014-12-05 2016-06-09 Acerta Pharma B.V. Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment
SG11201704808VA (en) 2014-12-18 2017-07-28 Principia Biopharma Inc Treatment of pemphigus
WO2016106627A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
WO2016161571A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. Indazole and azaindazole btk inhibitors
WO2016192074A1 (en) * 2015-06-04 2016-12-08 Merck Sharp & Dohme Corp. Btk inhibitors
US20180305350A1 (en) 2015-06-24 2018-10-25 Principia Biopharma Inc. Tyrosine kinase inhibitors
IL293821A (en) 2015-07-02 2022-08-01 Acerta Pharma Bv Solid forms and formulations of (S)-4-(8-amino-3-(1-(but-2-aminoyl)pyrrolidine-2-yl)imidazo[5,1-yl]pyrazin-1-yl)-en- (pyridine-2-yl)benzamide
US20190008859A1 (en) 2015-08-21 2019-01-10 Acerta Pharma B.V. Therapeutic Combinations of a MEK Inhibitor and a BTK Inhibitor
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EP3402503B1 (en) 2016-01-13 2020-10-21 Acerta Pharma B.V. Therapeutic combinations of an antifolate and a btk inhibitor
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
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US11554118B2 (en) * 2017-03-22 2023-01-17 Xibin Liao Bruton's tyrosine kinase inhibitors
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Also Published As

Publication number Publication date
WO2013010869A1 (en) 2013-01-24
AU2012285988B2 (en) 2017-05-25
JP2014522860A (ja) 2014-09-08
EP2734523A1 (en) 2014-05-28
AU2012285988A1 (en) 2014-01-30
US20140155406A1 (en) 2014-06-05

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20180711