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HRP20230379T1 - TETRAHIDROPIRANIL AMINO-PIROLOPIRIMIDINON ZA PRIMJENU U LIJEČENJU POREMEĆAJA POSREDOVANIH BTK-om - Google Patents

TETRAHIDROPIRANIL AMINO-PIROLOPIRIMIDINON ZA PRIMJENU U LIJEČENJU POREMEĆAJA POSREDOVANIH BTK-om Download PDF

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Publication number
HRP20230379T1
HRP20230379T1 HRP20230379TT HRP20230379T HRP20230379T1 HR P20230379 T1 HRP20230379 T1 HR P20230379T1 HR P20230379T T HRP20230379T T HR P20230379TT HR P20230379 T HRP20230379 T HR P20230379T HR P20230379 T1 HRP20230379 T1 HR P20230379T1
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HR
Croatia
Prior art keywords
compound
cancer
use according
lymphoma
btk
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HRP20230379TT
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English (en)
Inventor
Jean-Marc Lapierre
Sudharshan Eathiraj
Nivedita Namdev
Brian Schwartz
Yusuke Ota
Takayuki Momose
Tomoyuki Tsunemi
Hiroaki Inagaki
Kiyoshi Nakayama
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Arqule, 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.)
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Publication date
Application filed by Arqule, Inc. filed Critical Arqule, Inc.
Publication of HRP20230379T1 publication Critical patent/HRP20230379T1/hr

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    • 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
    • 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
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic 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)

Claims (17)

1. Spoj Formule (I): [image] ili farmaceutski prihvatljiva sol, tautomer, solvat, ili polimorf istog, za primjenu u postupku liječenja poremećaja posredovanog BTK-om ili moduliranja BTK, pri čemu BTK je mutant BTK, poželjno BTK C481S mutant.
2. Spoj za primjenu prema zahtjevu 1, pri čemu spoj je Formule (I): [image] ili farmaceutski prihvatljiva sol istog.
3. Spoj za primjenu prema zahtjevu 1, pri čemu spoj je Formule (I): [image]
4. Spoj za primjenu prema zahtjevu 1, pri čemu je spoj prisutan kao farmaceutska kompozicija koja sadrži spoj ili farmaceutski prihvatljivu sol, tautomer, solvat, ili polimorf istog, i farmaceutski prihvatljiv razblaživač, ekscipijens ili nosač.
5. Spoj za primjenu u skladu sa zahtjevom 1, pri čemu je poremećaj posredovan BTK-om odabran od imunoloških poremećaja, raka, kardiovaskularnih bolesti, virusnih infekcija, inflamacije, poremećaja metabolizma/endokrine funkcije i neuroloških poremećaja.
6. Spoj za primjenu u skladu sa zahtjevom 5, pri čemu je rak odabran od raka dojke, jajnika, grlića materice, prostate, testisa, genitourinarnog trakta, jednjaka, larinksa, želuca, kože, pluća, kosti, kolona, gušterače, tiroidne žlijezde, bilijarnog trakta, vlasastih stanica, bukalne šupljine, nazofaringealnog, ždrijela, usne, jezika, usta, tankog crijeva, kolon-rektuma, debelog crijeva, rektuma, mozga i centralnog živčanog sustava, bronhija, jetre, intrahepatičnog žučnog kanala, bubrega i bubrežne karlice, mokraćnog mjehura, tijela materice, grlića materice, ili usne duplje, glioblastoma, neuroblastoma, keratoakantoma, epidermoidnog karcinoma, krupnostaničnog karcinoma, nesitnostaničnog karcinoma pluća (NSCLC), sitnostaničnog karcinoma, adenokarcinoma pluća, adenoma, adenokarcinoma, folikularnog karcinoma, nediferenciranog karcinoma, papilarnog karcinoma, seminoma, melanoma, sarkoma, karcinoma mjehura, karcinoma jetre, karcinoma bubrega, mijeloidnih poremećaja, limfoma, Hodgkinove leukemije, hepatocelularnog raka, glioma/glioblastoma, endometrijalnog raka, multiplog mijeloma, akutne mijelogene leukemije, kronične mijelogene leukemije, limfocitne leukemije, kronične limfoidne leukemije (CLL), mijeloidne leukemije, ne-Hodgkinovog limfoma, i viloznog adenoma kolona.
7. Spoj za primjenu u skladu sa zahtjevom 6, pri čemu rak je kronična limfoidna leukemija (CLL).
8. Spoj za primjenu u skladu sa zahtjevom 6, pri čemu rak je limfom.
9. Spoj za primjenu u skladu sa zahtjevom 8, pri čemu limfom je ne-Hodgkinov limfom.
10. Spoj za primjenu u skladu sa zahtjevom 8, pri čemu limfom je B-stanični limfom.
11. Spoj za primjenu u skladu sa zahtjevom 8, pri čemu limfom je anaplastični limfom krupnih stanica, primarni limfom centralnog živčanog sustava ili Waldenströmova makroglobulinemija.
12. Spoj za primjenu u skladu sa zahtjevom 6, pri čemu rak je mijeloidni poremećaji ili mijeloidna leukemija.
13. Spoj za primjenu u skladu sa zahtjevom 6, pri čemu je rak akutna mijeloidna leukemija.
14. Spoj za primjenu u skladu sa zahtjevom 6, pri čemu rak je multipli mijelom.
15. Spoj za primjenu u skladu sa zahtjevom 6, pri čemu rak je limfocitna leukemija.
16. Spoj za primjenu u skladu sa zahtjevom 6, pri čemu rak je sarkom ili tumor mozga.
17. Spoj za primjenu u skladu sa zahtjevom 5, pri čemu je poremećaj posredovan BTK-om reumatoidni artritis, sustavna i lokalna inflamacija, artritis, inflamacija povezana sa imuno supresijom, odbacivanje transplantiranog organa, alergije, ulcerativni kolitis, Kronova bolest, dermatitis, astma, sustavni eritematozni lupus, Sjögrenov sindrom, multipla skleroza, skleroderma/sustavna skleroza, idiopatska trombocitopenična purpura (ITP), vaskulitis povezan sa anti-neutrofilnim citoplazmatskim antitijelima (ANCA), kronična opstruktivna plućna bolest (COPD), ili psorijaza.
HRP20230379TT 2015-12-23 2015-12-23 TETRAHIDROPIRANIL AMINO-PIROLOPIRIMIDINON ZA PRIMJENU U LIJEČENJU POREMEĆAJA POSREDOVANIH BTK-om HRP20230379T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP21165852.1A EP3882250B1 (en) 2015-12-23 2015-12-23 Tetrahydropyranyl amino-pyrrolopyrimidinone for use in treating btk-mediated disorders
PCT/US2015/000285 WO2017111787A1 (en) 2015-12-23 2015-12-23 Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof

Publications (1)

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HRP20230379T1 true HRP20230379T1 (hr) 2023-06-23

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HRP20230379TT HRP20230379T1 (hr) 2015-12-23 2015-12-23 TETRAHIDROPIRANIL AMINO-PIROLOPIRIMIDINON ZA PRIMJENU U LIJEČENJU POREMEĆAJA POSREDOVANIH BTK-om
HRP20210844TT HRP20210844T1 (hr) 2015-12-23 2021-05-26 Tetrahidropiranil amino-pirolopirimidinon i postupci njegove primjene

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EP (2) EP3394065B1 (hr)
JP (1) JP6634520B2 (hr)
KR (2) KR102547188B1 (hr)
CN (2) CN113307811B (hr)
AU (3) AU2015417922B2 (hr)
CA (1) CA3008446C (hr)
CY (1) CY1124210T1 (hr)
DK (2) DK3394065T3 (hr)
ES (2) ES2868884T3 (hr)
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HU (2) HUE061761T2 (hr)
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LT (2) LT3882250T (hr)
MA (1) MA56553B1 (hr)
MD (1) MD3882250T2 (hr)
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SA (1) SA518391836B1 (hr)
SG (1) SG11201805154YA (hr)
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CN112812100B (zh) * 2019-11-18 2022-04-05 四川海思科制药有限公司 一种具有降解btk激酶的化合物及其制备方法和药学上的应用
JP7011638B2 (ja) * 2019-12-16 2022-02-10 アークル インコーポレイテッド テトラヒドロピラニルアミノ-ピロロピリミジノンおよびその使用の方法
CN112608318B (zh) * 2019-12-16 2023-09-08 成都海博为药业有限公司 一种作为蛋白质激酶抑制剂的化合物及其用途
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JP2025500886A (ja) 2021-12-14 2025-01-15 クロスファイアー オンコロジー ホールディング ビー.ヴイ. 大環状btk阻害剤
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CN115894500B (zh) * 2022-11-02 2024-05-28 中国药科大学 一种作为btk激酶抑制剂的化合物及其制备方法与用途
CN118702697A (zh) * 2023-03-18 2024-09-27 山东新时代药业有限公司 苯甲酰基吡咯并嘧啶类衍生物及其用途和制备方法
CN116375715A (zh) * 2023-04-06 2023-07-04 中国药科大学 一种作为非共价btk激酶抑制剂的化合物及其生物用途
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WO2024245577A1 (en) 2023-06-02 2024-12-05 Netherlands Translational Research Center Holding B.V. Therapeutic combinations of an irreversible btk inhibitor and a reversible btk inhibitor
WO2024245578A1 (en) 2023-06-02 2024-12-05 Netherlands Translational Research Center Holding B.V. Therapeutic combinations of an irreversible btk inhibitor and a macrocyclic reversible btk inhibitor
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EP3882250B1 (en) 2023-02-15
FI3882250T3 (fi) 2023-04-27
MA56553A (fr) 2022-04-27
RU2018126793A3 (hr) 2020-01-23
EP3394065B1 (en) 2021-04-07
CN108699062A (zh) 2018-10-23
KR102547188B1 (ko) 2023-06-26
ES2942743T3 (es) 2023-06-06
EP3394065A1 (en) 2018-10-31
KR102746900B1 (ko) 2024-12-24
RS61887B1 (sr) 2021-06-30
IL282572B (en) 2022-04-01
IL259938A (en) 2018-07-31
EP3882250A1 (en) 2021-09-22
PT3394065T (pt) 2021-05-06
CN113307811A (zh) 2021-08-27
PL3882250T3 (pl) 2023-09-11
PL3394065T3 (pl) 2021-08-02
AU2019201737A1 (en) 2019-04-04
WO2017111787A1 (en) 2017-06-29
MX2018007815A (es) 2019-07-04
JP2018538349A (ja) 2018-12-27
SA518391836B1 (ar) 2022-06-19
RS64141B1 (sr) 2023-05-31
DK3394065T3 (da) 2021-05-31
EP3394065A4 (en) 2019-07-10
AU2015417922A1 (en) 2018-06-28
SI3394065T1 (sl) 2021-08-31
RU2715421C2 (ru) 2020-02-28
CA3008446A1 (en) 2017-06-29
CN108699062B (zh) 2021-06-29
HUE061761T2 (hu) 2023-08-28
AU2019201737B2 (en) 2020-03-05
SI3882250T1 (sl) 2023-07-31
KR20180096753A (ko) 2018-08-29
JP6634520B2 (ja) 2020-01-22
BR112018012828A2 (pt) 2018-12-04
CA3008446C (en) 2023-10-10
AU2020203690A1 (en) 2020-06-25
IL259938B (en) 2021-05-31
ES2868884T3 (es) 2021-10-22
MA56553B1 (fr) 2023-04-28
SG11201805154YA (en) 2018-07-30
PH12018501390B1 (en) 2022-06-10
MY193177A (en) 2022-09-26
CN113307811B (zh) 2023-11-14
RU2018126793A (ru) 2020-01-23
LT3882250T (lt) 2023-05-25
AU2015417922B2 (en) 2018-12-20
NZ743384A (en) 2024-05-31
PT3882250T (pt) 2023-04-21
HUE055221T2 (hu) 2021-11-29
CY1124210T1 (el) 2022-05-27
MD3882250T2 (ro) 2023-06-30
DK3882250T3 (da) 2023-05-22
PH12018501390A1 (en) 2019-02-27
HRP20210844T1 (hr) 2021-07-09
LT3394065T (lt) 2021-06-25
IL282572A (en) 2021-06-30
ZA201804091B (en) 2019-03-27
KR20230098690A (ko) 2023-07-04
AU2020203690B2 (en) 2021-08-05

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