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

Info

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
Authority
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
Other languages
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 and Dohme BV
Original Assignee
Merck Sharp and 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 and Dohme BV filed Critical Merck Sharp and Dohme BV
Publication of CA2841887A1 publication Critical patent/CA2841887A1/en
Abandoned legal-status Critical Current

Links

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

Landscapes

  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (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)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2710005T3 (pl) 2011-05-17 2017-07-31 Principia Biopharma Inc. Inhibitory kinazy tyrozynowej
US9376438B2 (en) 2011-05-17 2016-06-28 Principia Biopharma, Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
JP5826931B2 (ja) 2011-07-19 2015-12-02 メルク・シャープ・エンド・ドーム・ベー・フェー Ｂｔｋ阻害剤としての４−イミダゾピリダジン−１−イル−ベンズアミドおよび４−イミダゾトリアジン−１−イル−ベンズアミド
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
WO2014018567A1 (en) 2012-07-24 2014-01-30 Pharmacyclics, Inc. 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
CN104822663B (zh) * 2012-10-04 2017-03-08 犹他大学研究基金会 作为酪氨酸受体激酶btk抑制剂的取代的n‑(3‑(嘧啶‑4‑基)苯基)丙烯酰胺类似物
US20140206681A1 (en) 2013-01-23 2014-07-24 Ronald M. Kim Btk inhibitors
WO2014113942A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
US10328080B2 (en) 2013-12-05 2019-06-25 Acerta Pharma, B.V. Therapeutic combination of PI3K inhibitor and a BTK inhibitor
WO2015095102A1 (en) 2013-12-20 2015-06-25 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
KR20220027271A (ko) 2014-02-21 2022-03-07 프린시피아 바이오파마, 인코퍼레이티드 Btk 억제제의 염 및 고체 형태
WO2015136398A1 (en) 2014-03-12 2015-09-17 Novartis Ag Combination comprising a btk inhibitor and an akt inhibitor
WO2015181633A2 (en) 2014-04-11 2015-12-03 Acerta Pharma B.V. Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bruton's tyrosine kinase
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
US9949971B2 (en) 2014-06-17 2018-04-24 Acerta Pharma B.V. Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor and/or a JAK-2 inhibitor
TW201618783A (zh) 2014-08-07 2016-06-01 艾森塔製藥公司 以布魯頓(Bruton)氏酪胺酸激酶(BTK)佔據和BTK再合成速率為基礎之治療癌症、免疫和自體免疫疾病及發炎性疾病之方法
US20170239351A1 (en) 2014-08-11 2017-08-24 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, a PD-1 Inhibitor, and/or a PD-L1 Inhibitor
LT3179991T (lt) 2014-08-11 2021-11-10 Acerta Pharma B.V. Terapiniai btk inhibitoriaus ir bcl-2 inhibitoriaus deriniai
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
WO2016087994A1 (en) 2014-12-05 2016-06-09 Acerta Pharma B.V. Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment
CA2970723C (en) 2014-12-18 2023-09-05 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
MA42242A (fr) 2015-06-24 2018-05-02 Principia Biopharma Inc Inhibiteurs de la tyrosine kinase
HRP20211511T1 (hr) 2015-07-02 2021-12-24 Acerta Pharma B.V. Čvrsti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida
US20190008859A1 (en) 2015-08-21 2019-01-10 Acerta Pharma B.V. Therapeutic Combinations of a MEK Inhibitor and a BTK Inhibitor
US20190022092A1 (en) 2015-09-15 2019-01-24 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor and a GITR Binding Molecule, a 4-1BB Agonist, or an OX40 Agonist
MA44909A (fr) 2015-09-15 2018-07-25 Acerta Pharma Bv Association thérapeutique d'un inhibiteur du cd19 et d'un inhibiteur de la btk
WO2017122175A1 (en) 2016-01-13 2017-07-20 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
WO2018005849A1 (en) 2016-06-29 2018-01-04 Principia Biopharma Inc. Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
ES2856248T3 (es) 2016-12-21 2021-09-27 Acerta Pharma Bv Inhibidores de imidazopirazina de la tirosina quinasa de Bruton
WO2018134786A1 (en) 2017-01-19 2018-07-26 Acerta Pharma B.V. Compositions and methods for the assessment of drug target occupancy for bruton's tyrosine kinase
TWI754011B (zh) 2017-02-24 2022-02-01 美商基利科學股份有限公司 布魯頓氏酪胺酸激酶之抑制劑
US10314844B2 (en) 2017-02-24 2019-06-11 Gilead Sciences, Inc. Inhibitors of Bruton's tyrosine kinase
JP7219902B2 (ja) * 2017-03-22 2023-02-09 スジョウ・バイジブゴン・ファーマスーティカル・テクノロジー・カンパニー・リミテッド ブルトン型チロシンキナーゼ阻害剤
EA037031B1 (ru) * 2017-10-06 2021-01-28 Асерта Фарма Б.В. Имидазопиразиновые ингибиторы тирозинкиназы брутона
WO2019090269A1 (en) * 2017-11-06 2019-05-09 Peng Wang Processes to produce acalabrutinib
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
TWI877239B (zh) 2019-10-14 2025-03-21 美商普林斯匹亞生物製藥公司 藉由投予(R)-2-[3-[4-胺基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧呾-3-基)哌-1-基]戊-2-烯腈來治療免疫血小板減少症之方法
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
BR112022014149A2 (pt) 2020-01-22 2022-09-27 Principia Biopharma Inc Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenóxi-fenil)-1h-pirazolo[3,4-d]pirimidina-1-il]piperidina-1-carbonil]-4-metil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enenitrila
AU2022380979A1 (en) 2021-11-02 2024-06-06 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2630271C (en) * 2005-11-17 2014-04-08 Osi Pharmaceuticals, Inc. Fused bicyclic mtor inhibitors
EA017865B1 (ru) * 2007-03-28 2013-03-29 Фармасайкликс, Инк. Ингибиторы тирозинкиназы брутона
EP2424368B1 (en) * 2009-04-29 2014-12-31 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
CA2787291C (en) * 2010-02-08 2016-04-19 Msd Oss B.V. 8-methyl-1-phenyl-imidazol[1,5-a]pyrazine compounds

Also Published As

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

Similar Documents

Publication Publication Date Title
AU2012285988B2 (en) 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides Btk-inhibitors
AU2017279778B2 (en) 4 - imidazopyridazin- 1 -yl-benzamides and 4 - imidazotriazin- 1 - yl - benzamides as Btk- inhibitors
HK40096146A (en) (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-2-methoxy-n-(pyridin-2-yl)benzamide as btk-inhibitor
NZ716110B2 (en) 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk-inhibitors
HK1192752A (en) 4 - imidazopyridazin- 1 -yl-benzamides and 4 - imidazotriazin- 1 - yl - benzamides as btk- inhibitors
HK1192752B (en) 4 - imidazopyridazin- 1 -yl-benzamides and 4 - imidazotriazin- 1 - yl - benzamides as btk- inhibitors
NZ620085B2 (en) 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk-inhibitors
HK40008890A (en) (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-2-methoxy-n-(pyridin-2-yl)benzamide as btk-inhibitor
HK40008890B (en) (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-2-methoxy-n-(pyridin-2-yl)benzamide as btk-inhibitor
HK40026806B (en) 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk-inhibitors
HK40026806A (en) 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk-inhibitors

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20180711