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HRP20240101T1 - Supstituirani heterociklil derivati kao cdk inhibitori - Google Patents

Supstituirani heterociklil derivati kao cdk inhibitori Download PDF

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Publication number
HRP20240101T1
HRP20240101T1 HRP20240101TT HRP20240101T HRP20240101T1 HR P20240101 T1 HRP20240101 T1 HR P20240101T1 HR P20240101T T HRP20240101T T HR P20240101TT HR P20240101 T HRP20240101 T HR P20240101T HR P20240101 T1 HRP20240101 T1 HR P20240101T1
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Croatia
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compound
pharmaceutically acceptable
compound according
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acceptable salt
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HRP20240101TT
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Susanta Samajdar
Ramulu Poddutoori
Chetan Pandit
Subhendu MUKHERJEE
Rajeev Goswami
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Aurigene Oncology Limited
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Publication of HRP20240101T1 publication Critical patent/HRP20240101T1/hr

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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/4965—Non-condensed pyrazines
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    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Claims (30)

1. Spoj formule (IB): [image] Ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer; pri čemu, prsten B je fenil ili 5-14 člani heterociklil; R2 je vodik, (C1-C10)alkil ili (C3-C10)cikloalkil; R3 je vodik ili (C1-C10)alkil; alternativno, R2 zajedno s R3 zajedno s atomima prstena na koje su vezani tvori 5-7 člani prsten; R4 je pri svakom pojavljivanju halo, (C1-C10)alkil ili halo(C1-C10)alkil; R5 je [image] ili [image] pri čemu je R5' vodik, (C1-C10)alkil, (C1-C10)alkoksialkil ili -(CH2)1-3-NRaRb; R5" je H ili (C1-C10)alkil; Ra i Rb su svaki neovisno vodik, (C1-C10)alkil, (C1-C10)alkoksi ili (C1-C10)alkoksialkil; alternativno, Ra i Rb zajedno s atomom dušika na koji su vezani tvore izborno supstituirani 5-6 člani prsten koji sadrži 0-2 dodatna heteroatoma koji su neovisno N, O ili S; pri čemu je izborni supstituent jedan ili više halo, (C1-C10)alkil, hidroksi, cijano, cijano(C1-C10)alkil, halo(C1-C10)alkil, (C1-C10)alkoksi, (C1-C10)alkoksialkil -COOH ili -COO-(C1-C10)alkil; R6 je pri svakom pojavljivanju halo, (C1-C10)alkil, (C1-C10)alkoksi ili halo(C1-C10)alkil; Li je *-CRcRd-C(O)- ili ga nema; pri čemu je * točka vezivanja s fenilnim prstenom; Rc i Rd su neovisno vodik ili (C1-C10)alkil; alternativno, Rc i Rd zajedno s atomom ugljika na koji su vezani tvore (C3-C10)cikloalkilni prsten; L2 je -C(O)NH- ili ga nema; m je 0, 1 ili 2; p je 1;i q je 0 do 3.
2. Spoj prema patentnom zahtjevu 1, koji ima formulu (ID): [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
3. Spoj prema patentnom zahtjevu 1, koji ima formulu (IE): [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer; pri čemu, L1 je *-CRcRd-C(O)-; pri čemu je * točka vezivanja s fenilnim prstenom.
4. Spoj prema patentnom zahtjevu 1, koji ima formulu (IF): [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
5. Spoj prema patentnim zahtjevima 1 ili 2, pri čemu je prsten B piperidinil, piridinil, piperazinil, pirazolil, morfolinil, indolinil ili pirolidinil.
6. Spoj prema patentnim zahtjevima 1 do 4, pri čemu je R5 [image]
7. Spoj prema patentnom zahtjevu 1, pri čemu je L2 *-C(O)NH-; pri čemu je * točka vezivanja s prstenom B.
8. Spoj prema patentnom zahtjevu 1, izabran od [image] [image] [image] [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
9. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
10. Spoj prema patentnom zahtjevu 1, pri čemu je spoj (E)-N-(5-(3-(1-((5-ciklopropil-1H-pirazol-3-il)amino)-1-oksopropan-2-il)fenil)piridin-2-il)-4-((S)-3-fluoropirolidin-1-il)but-2-enamid ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
11. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
12. Spoj prema patentnom zahtjevu 1, pri čemu je spoj N-(5-(3-(1-((5-ciklopropil-1H-pirazol-3-il)amino)-1-oksopropan-2-il)fenil)piridin-2-il)akrilamid ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
13. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
14. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
15. Spoj prema patentnom zahtjevu 1, pri čemu je spoj (E)-N-(5-(3-(1-((5-ciklopropil-1H-pirazol-3-il)amino)-1-oksopropan-2-il)fenil)piridin-2-il)-4-morfolinobut-2-enamid ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
16. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
17. Spoj prema patentnom zahtjevu 1, pri čemu je spoj (E)-N-(5-(3-(1-((5-ciklopropil-1H-pirazol-3-il)amino)-1-oksopropan-2-il)-fenil)piridin-2-il)-4-(pirolidin-1-il)but-2-enamid ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
18. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
19. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
20. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
21. Spoj prema patentnom zahtjevu 1, pri čemu je spoj, spoj formule: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer.
22. Spoj prema patentnom zahtjevu 1, pri čemu je enantiomer (E)-N-(5-(3-(1-((5-ciklopropil-1H-pirazol-3-il)amino)-3-metil-1-oksobutan-2-il)fenil)piridin-2-il)-4-morfolinobut-2-enamid.
23. Spoj prema patentnom zahtjevu 1, pri čemu je enantiomer (E)-N-(5-(3-(1-((5-ciklopropil-1H-pirazol-3-il)amino)-3-metil-1-oksobutan-2-il)fenil)piridin-2-il)-4-morfolinobut-2-enamid ili njegova farmaceutski prihvatljiva sol.
24. Farmaceutski sastav koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 23, ili njegovu farmaceutski prihvatljivu sol ili stereoizomer i najmanje jednu farmaceutski prihvatljivu pomoćnu tvar.
25. Farmaceutski sastav prema patentnom zahtjevu 24 za upotrebu u liječenju subjekta koji boluje od bolesti i/ili poremećaja povezanih s aberantnom aktivnošću selektivnih transkripcijskih CDK-a, pri čemu su bolesti i/ili poremećaji posredovani selektivnim transkripcijskim CDK-ima koji su izabrani iz skupine koja se sastoji od raka, upalnog poremećaja, autoupalnog poremećaja i zarazne bolesti.
26. Spoj prema bilo kojem od patentnih zahtjeva 1 do 23 za upotrebu u liječenju raka.
27. Spoj prema bilo kojem od patentnih zahtjeva 1 do 23 za uporabu u liječenju bolesti i/ili poremećaja posredovanih selektivnim transkripcijskim CDK-ima kod ispitanika, pri čemu bolesti i/ili poremećaji posredovani selektivnim transkripcijskim CDK-ima su izabrani iz skupine koja se sastoji od raka, upalnog poremećaja, autoupalnog poremećaj i zarazne bolesti.
28. Spoj za upotrebu prema patentnom zahtjevu 27, pri čemu su selektivni transkripcijski CDK-i CDK7, CDK9, CDK12, CDK13 ili CDK18.
29. Spoj za upotrebu prema patentnom zahtjevu 27, pri čemu je rak izabran iz skupine koju čine karcinom, uključujući karcinom dojke, jetra, pluća, debelog crijeva, bubrega, mokraćnog mjehura, uključujući rak pluća malih stanica, rak pluća nemalih stanica, glave i vrata, štitnjače, jednjaka, želuca, gušterače, jajnika, žučnog mjehura, cerviksa, prostate i kože, uključujući karcinom skvamoznih stanica; hematopoetske tumore limfoidne loze, uključujući leukemiju, akutnu limfoblastičnu leukemiju, akutnu limfocitnu leukemiju, Hodgkinov limfom, ne-Hodgkinov limfom, B-stanični limfom, T-stanični limfom, limfom vlasastih stanica, mijelom, limfom stanica plašta i Burkettov limfom; hematopoetske tumore mijeloidne loze, uključujući akutne i kronične mijelogene leukemije, mijelodisplastični sindrom i promijelocitnu leukemiju; tumore mezenhimalnog porijekla, uključujući fibrosarkom i rabdomiosarkom; tumore središnjeg i perifernog živčanog sustava, uključujući astrocitome, neuroblastome, gliome i švanome; i druge tumore, uključujući seminom, melanom, osteosarkom, teratokarcinom, keratoakantom, pigmentnu kserodermu, folikularni karcinom štitnjače i Kaposijev sarkom.
30. Spoj za upotrebu prema patentnim zahtjevima 27 ili 28, zajedno s jednim ili više dodatnih kemoterapijskih sredstava neovisno odabranih između anti-proliferativnih sredstava, sredstava protiv raka, sredstava za suzbijanje imuniteta i sredstava za ublažavanje bolova.
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Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016142855A2 (en) * 2015-03-09 2016-09-15 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
MY190459A (en) * 2015-06-04 2022-04-21 Aurigene Discovery Tech Ltd Substituted heterocyclyl derivatives as cdk inhibitors
GB201617548D0 (en) 2016-10-17 2016-11-30 Linnane Pharma Ab Novel biological factor
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
AU2018380132B2 (en) 2017-12-06 2023-11-09 Lin Bioscience, Inc. Tubulin inhibitors
US11472774B2 (en) 2018-02-01 2022-10-18 The University Of Sydney Anti-cancer compounds
CA3095568A1 (en) * 2018-03-29 2019-10-03 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP3774768A4 (en) * 2018-04-04 2022-01-05 Aurigene Discovery Technologies Limited SUBSTITUTED PYRAZOLE DERIVATIVES AS SELECTIVE CDK12 / 13 INHIBITORS
EP3787629A4 (en) 2018-05-02 2022-01-05 Kinnate Biopharma Inc. INHIBITORS OF CYCLINE-DEPENDENT KINASES
CN110590747B (zh) * 2018-06-12 2022-03-22 隆泰申医药科技(南京)有限公司 一种化合物、其制备方法、药物组合物和应用
WO2020005807A1 (en) * 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
EP3813819A4 (en) 2018-06-29 2022-08-17 Kinnate Biopharma Inc. CYCLIN DEPENDENT KINASE INHIBITORS
MX2021002456A (es) * 2018-09-17 2021-06-15 Yungjin Pharmaceutical Co Ltd Nuevos derivados de tiazol y sus sales farmaceuticamente aceptables.
WO2020202001A1 (en) 2019-04-01 2020-10-08 Aurigene Discovery Technologies Limited Substituted 5-cyclopropyl-1h-pyrazol-3-yl-amine derivatives as selective cdk12/13 inhibitors
CN110845474B (zh) * 2019-11-07 2021-01-12 四川大学 一种靶向i型prmt的化合物及其制备方法和应用
WO2021182918A1 (ko) * 2020-03-13 2021-09-16 영진약품 주식회사 티아졸 유도체 또는 이의 약제학적으로 허용가능한 염을 포함하는 암의 예방 또는 치료용 약학 조성물
KR102335637B1 (ko) * 2020-03-13 2021-12-06 영진약품 주식회사 신규한 cdk7 억제 화합물 및 이의 약제학적으로 허용가능한 염
TWI783480B (zh) * 2020-05-27 2022-11-11 美商美國禮來大藥廠 用於抑制cdk7之化合物
US20240016811A1 (en) * 2020-10-22 2024-01-18 Aurigene Oncology Limited Cancer therapy using a combination of cdk7 inhibitor with an anti-microtubule agent
TW202241881A (zh) 2020-12-18 2022-11-01 印度商阿瑞吉探索科技股份有限公司 Cdk抑制劑之共晶體
JP2024515760A (ja) * 2021-04-27 2024-04-10 オーリジーン オンコロジー リミテッド Ｃｄｋ阻害剤を調製するためのプロセス
JP2024523892A (ja) * 2021-06-16 2024-07-02 ブループリント メディシンズ コーポレイション Ｃｄｋ２阻害剤としての置換ピリミジニルーピラゾール
UY39832A (es) 2021-06-28 2023-01-31 Blueprint Medicines Corp Inhibidores de cdk2
TW202327583A (zh) * 2021-12-06 2023-07-16 美商艾克塞里克斯公司 使用ｃｄｋ７抑制劑治療癌症之方法
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
JP7557090B2 (ja) 2022-05-11 2024-09-26 株式会社前川製作所 削ぎ切り装置、及び、ワークの削ぎ切り方法
WO2023224961A1 (en) 2022-05-16 2023-11-23 Exelixis, Inc. Cancer therapy using a combination of a cdk7 inhibitor with an oral serd
CN115093397B (zh) * 2022-06-07 2023-09-05 自贡市第三人民医院 一种用于治疗肿瘤的化合物、合成方法及应用
WO2024066984A1 (zh) * 2022-09-30 2024-04-04 楚浦创制（武汉）医药科技有限公司 三并环类衍生物、药物组合物以及应用
WO2024140653A1 (zh) * 2022-12-27 2024-07-04 南京圣和药业股份有限公司 选择性cdk12/13抑制剂及其应用

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS57169465A (en) * 1981-04-13 1982-10-19 Showa Denko Kk Pyrazole derivative, its preparation and herbicide
US6399627B1 (en) 1999-02-11 2002-06-04 Cor Therapeutics, Inc. Inhibitors of factor Xa
DK1202733T3 (da) 1999-08-12 2005-10-31 Pharmacia Italia Spa 3(5)-amino-pyrazolderivater, fremgangsmåde til deres fremstilling og deres anvendelse som antitumormidler
US7541354B2 (en) * 2000-08-10 2009-06-02 Pfizer Italia S.R.L. Bicyclo-pyrazoles
US6455559B1 (en) 2001-07-19 2002-09-24 Pharmacia Italia S.P.A. Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents
JP2004517840A (ja) * 2000-11-27 2004-06-17 フアルマシア・イタリア・エツセ・ピー・アー フェニルアセトアミド−ピラゾール誘導体およびそれの抗腫瘍薬としての使用
DE10148618B4 (de) * 2001-09-25 2007-05-03 Schering Ag Substituierte N-(1,4,5,6-Tetrahydro-cyclopentapyrazol-3-yl)-Derivate, deren Herstellung und Verwendung als Arzneimittel
EP1673336B1 (en) 2003-08-21 2014-06-04 Merck Canada Inc. Cathepsin cysteine protease inhibitors
JP2008526723A (ja) * 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Ｃｄｋ、ｇｓｋ及びオーロラキナーゼの活性を調節するピラゾール誘導体
KR101334511B1 (ko) 2004-12-30 2013-11-29 아스텍스 테라퓨틱스 리미티드 Ｃｄｋ, ｇｓｋ 및 오로라 키나아제의 활성을 조절하는피라졸 화합물
JP2008528469A (ja) 2005-01-21 2008-07-31 アステックス・セラピューティクス・リミテッド ピラゾールキナーゼ阻害剤およびさらなる抗癌剤の組合せ剤
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
GT200600457A (es) 2005-10-13 2007-04-27 Aventis Pharma Inc Sal de fosfato dihidrogeno como antagonistas del receptor de prostaglandina d2
US20110269740A1 (en) * 2008-07-02 2011-11-03 Ambit Biosciences Corporation Jak kinase modulating compounds and methods of use thereof
EP2313758B1 (en) 2008-07-17 2012-02-01 Koninklijke Philips Electronics N.V. Nanopore device and a method for nucleic acid analysis
MX2011006332A (es) 2008-12-23 2011-06-27 Abbott Lab Compuestos antivirales.
FR2943058B1 (fr) 2009-03-11 2011-06-03 Centre Nat Rech Scient Derives de pyrazolo°1,5-a!-1,3,5-triazines, leur preparation et leur application en therapeutique.
EP2241619A1 (en) * 2009-04-17 2010-10-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Development of fluorescently P-loop labeled kinases for screening of inhibitors
EP2822935B1 (en) * 2011-11-17 2019-05-15 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US9657006B2 (en) 2013-06-13 2017-05-23 Bristol-Myers Squibb Company Macrocyclic factor VIIa inhibitors
SG11201601341QA (en) 2013-08-30 2016-03-30 Ambit Biosciences Corp Biaryl acetamide compounds and methods of use thereof
DK3060550T3 (da) 2013-10-21 2019-07-22 Merck Patent Gmbh Heteroarylforbindelser som btk-inhibitorer og anvendelser deraf
US10336760B2 (en) 2014-04-05 2019-07-02 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
FR3025075A1 (fr) * 2014-08-28 2016-03-04 Oreal Nouveau dispositif de soin et/ou maquillage comprenant une composition d’architecture gel/gel
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
MY190459A (en) * 2015-06-04 2022-04-21 Aurigene Discovery Tech Ltd Substituted heterocyclyl derivatives as cdk inhibitors

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