HRP20221152T1 - Spojevi korisni u inhibiranju cdk7 - Google Patents

Spojevi korisni u inhibiranju cdk7 Download PDF

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Publication number
HRP20221152T1
HRP20221152T1 HRP20221152TT HRP20221152T HRP20221152T1 HR P20221152 T1 HRP20221152 T1 HR P20221152T1 HR P20221152T T HRP20221152T T HR P20221152TT HR P20221152 T HRP20221152 T HR P20221152T HR P20221152 T1 HRP20221152 T1 HR P20221152T1
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Croatia
Prior art keywords
compound
salt
cancer
patient
use according
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HRP20221152TT
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English (en)
Inventor
David Andrew Coates
Carlos Montero
Bharvin Kumar Rameschandra Patel
David Michael Remick
Vipin Yadav
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Eli Lilly And Company
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Publication of HRP20221152T1 publication Critical patent/HRP20221152T1/hr

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    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (24)

1. Spoj, naznačen time što ima formulu (I) [image] , ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu (II) [image] , ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time što ima formulu (II) [image] .
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu (III) [image] , ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što ima formulu (III) [image] .
6. Spoj, ili sol, u skladu s patentnim zahtjevom 2, naznačen time što je hidrat hidrokloridne, besilatne ili hemiedisilatne soli.
7. Spoj, ili sol, u skladu s patentnim zahtjevom 4, naznačen time što je hidrat besilatne ili hemiedisilatne soli.
8. Spoj, ili sol, u skladu s patentnim zahtjevom 2, naznačen time što je u obliku kristalne soli.
9. Spoj, ili sol, u skladu s patentnim zahtjevom 8, koji je kristalni [(3S)-1-[(E)-4-(dimetilamino)but-2-enoil]pirolidin-3-il]-4-[(3-izopropil-5-metilpirazolo[1,5-a]pirimidin-7-il)amino]piperidin-1-karboksilat-besilat, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu koji ima karakteristične vrhove uz pomoć CuKα zračenja, u 2θ ± 0,2°, koji se pojavljuje na 21,5° u kombinaciji s jednim ili više vrhova koje se bira iz skupine kou čine 12,4°, 17,3°, te 15,8°.
10. Spoj, ili sol, u skladu s patentnim zahtjevom 8, koji je [(3S)-1-[(E)-4-(dimetilamino)but-2-enoil]pirolidin-3-il]-4-[(3-izopropil-5-metilpirazolo[1,5-a]pirimidin-7-il)amino]piperidin-1-karboksilat-hemiedisilat hidrat, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu koji ima karakteristične vrhove uz pomoć CuKα zračenja, u 2θ ± 0,2°, koji se pojavljuje na 18,5° u kombinaciji s jednim ili više vrhova koje se bira iz skupine kou čine 21,5°, 16,7°, te 15,2°.
11. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegovu farmaceutski prihvatljivu sol, u kombinaciji s jednim ili više farmaceutski prihvatljivih nosača, razrjeđivača ili pomoćnih sredstava.
12. Farmaceutski pripravak u skladu s patentnim zahtjevom 11, naznačen time što sadrži jedno ili više drugih terapijskih sredstava.
13. Spoj, ili njegova sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što je namijenjen upotrebi u terapiji.
14. Spoj ili njegova sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što je namijenjen upotrebi u postupku liječenja urotelijalnog raka, raka maternice, kolorektalnog raka, raka dojke, raka pluća, raka jajnika, raka želuca, hepatobilijarnog raka, raka gušterače, rakova vrata maternice, raka prostate, hematoloških rakova, sarkoma, rakova kože ili glioma.
15. Spoj, ili sol, namijenjen upotrebi u skladu s patentnim zahtjevom 14, naznačen time što je rak kolorektalni rak, rak dojke, rak pluća, rak jajnika ili rak želuca.
16. Spoj, ili sol, namijenjen upotrebi u skladu s bilo patentnim zahtjevom 14 ili 15, naznačen time što je rak rak dojke.
17. Spoj, ili njegova sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 13 do 16, naznačen time što postupak također uključuje provođenje analize in vitro na biološkom uzorku iz pacijenta, koji se sastoji u određivanju prisutnosti najmanje jedne inaktivirajuće mutacije u genima ARID1A, KMT2C, KMT2D i RB1, te u primjeni terapijske djelotvorne količine spoja, ili njegove soli, na pacijentu ako je prisutna najmanje jedna inaktivirajuća mutacija u bilo kojem od gena.
18. Spoj, ili njegova sol, namijenjen upotrebi u skladu s patentnim zahtjevom 17, naznačen time što je biološki uzorak uzorak tumora, a uzorak se analizira sekvencioniranjem genoma/DNA.
19. Spoj, ili njegova sol, namijenjen upotrebi u skladu s bilo patentnih zahtjeva 17 ili 18, naznačen time što se uzorak dobiva iz pacijenta prije prve primjene spoja, ili njegove soli, na pacijentu.
20. Spoj, ili njegova sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 13 do 19, naznačen time što se pacijenta bira za liječenje zbog toga što ima najmanje jednu inaktivirajuću mutaciju u genu ARID1A.
21. Spoj, ili njegova sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 13 do 19, naznačen time što se pacijenta bira za liječenje zbog toga što ima najmanje jednu inaktivirajuću mutaciju u genu KMT2C.
22. Spoj, ili njegova sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 13 do 19, naznačen time što se pacijenta bira za liječenje zbog toga što ima najmanje jednu inaktivirajuću mutaciju u genu KMT2D.
23. Spoj, ili njegova sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 13 do 19, naznačen time što se pacijenta bira za liječenje zbog toga što ima najmanje jednu inaktivirajuću mutaciju u genu RB1.
24. Spoj, ili njegova sol, namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 13 do 23, naznačen time što se spoj, ili njegovu sol, primjenjuje na pacijentu u dozi od otprilike 1 mg do 2 g.
HRP20221152TT 2017-11-16 2018-11-09 Spojevi korisni u inhibiranju cdk7 HRP20221152T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP17382778 2017-11-16
EP18382034 2018-01-23
EP18382546 2018-07-20
PCT/US2018/060025 WO2019099298A1 (en) 2017-11-16 2018-11-09 Compounds useful for inhibiting cdk7
EP18808599.7A EP3710446B1 (en) 2017-11-16 2018-11-09 Compounds useful for inhibiting cdk7

Publications (1)

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HRP20221152T1 true HRP20221152T1 (hr) 2022-11-25

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US (3) US10472370B2 (hr)
EP (1) EP3710446B1 (hr)
JP (1) JP6633254B2 (hr)
KR (1) KR102450727B1 (hr)
CN (1) CN111344292B (hr)
AU (1) AU2018369508B2 (hr)
BR (1) BR112020008253A2 (hr)
CA (1) CA3080910C (hr)
CL (1) CL2020001218A1 (hr)
CR (1) CR20200184A (hr)
DK (1) DK3710446T3 (hr)
DO (1) DOP2020000102A (hr)
EC (1) ECSP20025899A (hr)
ES (1) ES2925219T3 (hr)
HR (1) HRP20221152T1 (hr)
HU (1) HUE060078T2 (hr)
IL (1) IL274540B (hr)
JO (1) JOP20200122B1 (hr)
LT (1) LT3710446T (hr)
MD (1) MD3710446T2 (hr)
MX (1) MX2020004932A (hr)
MY (1) MY197700A (hr)
NZ (1) NZ763551A (hr)
PE (1) PE20210392A1 (hr)
PL (1) PL3710446T3 (hr)
RS (1) RS63530B1 (hr)
SA (1) SA520411990B1 (hr)
SG (1) SG11202003677UA (hr)
SI (1) SI3710446T1 (hr)
TW (1) TWI703149B (hr)
WO (1) WO2019099298A1 (hr)

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Publication number Priority date Publication date Assignee Title
EP3805218A1 (en) * 2014-04-05 2021-04-14 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
TWI703149B (zh) * 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物
JP2023501950A (ja) * 2019-10-29 2023-01-20 サイロス ファーマシューティカルズ, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤を用いてバイオマーカーにより特定された患者におけるがんを処置する方法
JP2023507028A (ja) 2019-12-20 2023-02-20 エボポイント、バイオサイエンシズ、カンパニー、リミテッド 複素環式化合物とその医薬組成物、調製方法、中間体及び使用
WO2022033552A1 (zh) * 2020-08-12 2022-02-17 隆泰申医药科技(南京) 有限公司 Cdk激酶抑制剂、其制备方法、药物组合物和应用
USD1004118S1 (en) 2021-08-31 2023-11-07 MerchSource, LLC Percussion massager
USD1004117S1 (en) 2021-08-31 2023-11-07 MerchSource, LLC Percussion massager
USD1004119S1 (en) 2021-08-31 2023-11-07 MerchSource, LLC Percussion massager
USD987844S1 (en) 2021-08-31 2023-05-30 MerchSource, LLC Percussion massager
USD994898S1 (en) 2021-11-17 2023-08-08 MerchSource, LLC Percussion massager
USD995812S1 (en) 2021-11-22 2023-08-15 MerchSource, LLC Percussion massager
USD1009292S1 (en) 2021-12-22 2023-12-26 MerchSource, LLC Percussion massager
USD1018881S1 (en) 2021-12-22 2024-03-19 MerchSource, LLC Percussion massager
USD1004121S1 (en) 2021-12-31 2023-11-07 MerchSource, LLC Pivoting percussion massager
USD1004122S1 (en) 2021-12-31 2023-11-07 MerchSource, LLC Pivoting percussion massager
CN114452391B (zh) * 2022-01-28 2023-08-25 深圳市泰尔康生物医药科技有限公司 Cdk16作为靶标在制备用于治疗三阴性乳腺癌的药物中的应用

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DE60313872T2 (de) * 2002-09-04 2008-01-17 Schering Corp. Pyrazoloä1,5-aüpyrimidine als hemmstoffe cyclin-abhängiger kinasen
GB201403093D0 (en) * 2014-02-21 2014-04-09 Cancer Rec Tech Ltd Therapeutic compounds and their use
EP3805218A1 (en) * 2014-04-05 2021-04-14 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3268000B1 (en) * 2015-03-09 2021-08-04 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
US10550121B2 (en) 2015-03-27 2020-02-04 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
KR20180041112A (ko) 2015-06-04 2018-04-23 오리진 디스커버리 테크놀로지스 리미티드 Cdk 억제제로서의 치환된 헤테로사이클릴 유도체
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
TWI703149B (zh) * 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物

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CN111344292A (zh) 2020-06-26
KR20200070323A (ko) 2020-06-17
CL2020001218A1 (es) 2020-08-21
PE20210392A1 (es) 2021-03-02
MX2020004932A (es) 2020-08-27
LT3710446T (lt) 2022-09-26
JOP20200122A1 (ar) 2020-05-20
MY197700A (en) 2023-07-06
PL3710446T3 (pl) 2022-10-10
ES2925219T3 (es) 2022-10-14
EP3710446A1 (en) 2020-09-23
MD3710446T2 (ro) 2022-12-31
CA3080910C (en) 2023-02-07
ECSP20025899A (es) 2020-06-30
RS63530B1 (sr) 2022-09-30
CA3080910A1 (en) 2019-05-23
JOP20200122B1 (ar) 2023-09-17
AU2018369508A1 (en) 2020-05-07
TWI703149B (zh) 2020-09-01
DOP2020000102A (es) 2020-08-31
US20200017513A1 (en) 2020-01-16
US10787460B2 (en) 2020-09-29
JP2019537616A (ja) 2019-12-26
CR20200184A (es) 2020-06-01
HUE060078T2 (hu) 2023-01-28
AU2018369508B2 (en) 2021-03-11
IL274540A (en) 2020-06-30
KR102450727B1 (ko) 2022-10-06
JP6633254B2 (ja) 2020-01-22
US20190144456A1 (en) 2019-05-16
SA520411990B1 (ar) 2022-07-24
WO2019099298A1 (en) 2019-05-23
US20210032257A1 (en) 2021-02-04
NZ763551A (en) 2021-12-24
US10472370B2 (en) 2019-11-12
IL274540B (en) 2022-06-01
EP3710446B1 (en) 2022-07-20
SI3710446T1 (sl) 2022-09-30
DK3710446T3 (da) 2022-08-01
SG11202003677UA (en) 2020-05-28
CN111344292B (zh) 2022-06-03
TW201930305A (zh) 2019-08-01
BR112020008253A2 (pt) 2020-11-17

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