PE20180530A1 - Derivados de amidas policiclicas como inhibidores de cdk9 - Google Patents

Derivados de amidas policiclicas como inhibidores de cdk9

Info

Publication number
PE20180530A1
PE20180530A1 PE2017002874A PE2017002874A PE20180530A1 PE 20180530 A1 PE20180530 A1 PE 20180530A1 PE 2017002874 A PE2017002874 A PE 2017002874A PE 2017002874 A PE2017002874 A PE 2017002874A PE 20180530 A1 PE20180530 A1 PE 20180530A1
Authority
PE
Peru
Prior art keywords
pyridin
lymphoma
tetrahydroimidazo
carboxamide
chloro
Prior art date
Application number
PE2017002874A
Other languages
English (en)
Inventor
Kurt Gordon Pike
Bernard Christophe Barlaam
Janet Hawkins
Savi Christopher De
Melissa Marie Vasbinder
Alexander Hird
Michelle Lamb
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of PE20180530A1 publication Critical patent/PE20180530A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • 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

Abstract

Se refiere a derivados de piridina o pirimidina de formula I, en donde: A es C(R5), N; R2 es heterocicloalquilo de 3-7 miembros, cicloalquilo de 3-7 miembros, cualquiera de ellos opcionalmente sustituido; y R4 es una de las formulas que se indica a continuacion. Estos compuestos inhiben CDK9 y pueden ser utiles en el tratamiento de enfermedades hiperproliferativas como el cancer, incluyendo trastornos hematologicos malignos como la leucemia mieloide aguda, mieloma multiple, leucemia linfocitica cronica, linfoma difuso de celulas B grandes, linfoma de Burkitt, linfoma folicular y tumores solidos como por ejemplo cancer de mama, pulmon, neuroblastoma y colon. Entre los compuestos preferidos tenemos los siguientes: (R)-N-(5-cloro-4-(5,6,7,8-tetrahidroimidazo[1,2-a]piridin-3-il)piridin-2-il)piperidin-3-carboxamida; (1S,3R)-3-acetamido de-N-(5-cloro-4-(5,6,7,8-tetrahidroimidazo[1,2-a]piridin-3-il)piridin-2-il)piperidin-3-carboxamida; entre otros.
PE2017002874A 2015-06-29 2016-06-27 Derivados de amidas policiclicas como inhibidores de cdk9 PE20180530A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562185852P 2015-06-29 2015-06-29

Publications (1)

Publication Number Publication Date
PE20180530A1 true PE20180530A1 (es) 2018-03-19

Family

ID=56292699

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002874A PE20180530A1 (es) 2015-06-29 2016-06-27 Derivados de amidas policiclicas como inhibidores de cdk9

Country Status (35)

Country Link
US (4) US9845331B2 (es)
EP (2) EP3539961B1 (es)
JP (1) JP6997627B2 (es)
CN (1) CN107873028B (es)
AR (1) AR105179A1 (es)
AU (1) AU2016286200B2 (es)
BR (1) BR122019013677B1 (es)
CA (1) CA2989499C (es)
CL (1) CL2017003306A1 (es)
CO (1) CO2017013713A2 (es)
CR (2) CR20210297A (es)
CY (2) CY1122111T1 (es)
DK (2) DK3313838T3 (es)
DO (2) DOP2017000295A (es)
EA (1) EA035383B1 (es)
ES (2) ES2902148T3 (es)
HR (2) HRP20211970T1 (es)
HU (2) HUE043440T2 (es)
IL (1) IL256393B (es)
LT (2) LT3539961T (es)
ME (1) ME03404B (es)
MX (1) MX371034B (es)
NI (1) NI201700174A (es)
PE (1) PE20180530A1 (es)
PH (1) PH12017502334A1 (es)
PL (2) PL3539961T3 (es)
PT (2) PT3313838T (es)
RS (2) RS62781B1 (es)
SI (2) SI3539961T1 (es)
SV (1) SV2017005598A (es)
TN (1) TN2017000486A1 (es)
TR (1) TR201909286T4 (es)
TW (1) TWI723028B (es)
WO (1) WO2017001354A1 (es)
ZA (1) ZA201800563B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2018335617B2 (en) 2017-09-25 2021-12-09 Astrazeneca Ab Combination of a BTK inhibitor and an inhibitor of CDK9 to treat cancer
EP3694506B1 (en) * 2017-10-09 2023-08-02 Merck Sharp & Dohme LLC Novel substituted phenyloxetane and phenyltetrahydrofuran compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
CN108129288B (zh) * 2017-12-27 2021-01-22 上海毕得医药科技股份有限公司 一种反式-3-羟基环丁基甲酸的合成方法
TW202344250A (zh) 2018-11-14 2023-11-16 瑞典商阿斯特捷利康公司 治療癌症之方法
CA3153531A1 (en) * 2019-09-11 2021-03-18 Prelude Therapeutics Incorporated Cdk inhibitors and their use as pharmaceuticals
JP7406008B2 (ja) * 2020-05-12 2023-12-26 蘇州阿尓脈生物科技有限公司 Cdk9阻害剤としての多環式アミド系誘導体、その調製方法及び用途
WO2021227906A1 (zh) 2020-05-12 2021-11-18 苏州阿尔脉生物科技有限公司 一种作为cdk抑制剂的吡啶乙酰胺类衍生物、其制备方法及用途
TW202216207A (zh) 2020-06-24 2022-05-01 英商阿斯特捷利康英國股份有限公司 抗體-藥物結合物及cdk9抑制劑之組合
WO2022028556A1 (zh) 2020-08-07 2022-02-10 南京药石科技股份有限公司 Cdk9抑制剂及其用途
TWI809330B (zh) * 2020-11-20 2023-07-21 大陸商勁方醫藥科技(上海)有限公司 Cdk9抑制劑的多晶型物及其製法和用途
CN115381824A (zh) * 2021-05-24 2022-11-25 石药集团中奇制药技术(石家庄)有限公司 周期蛋白依赖性激酶9抑制剂的用途
CN115381823A (zh) * 2021-05-24 2022-11-25 石药集团中奇制药技术(石家庄)有限公司 一种周期蛋白依赖性激酶9抑制剂的用途
CN117813289A (zh) * 2021-07-14 2024-04-02 上海海雁医药科技有限公司 吡唑衍生物及其中间体和制备方法
US20230279016A1 (en) * 2021-12-23 2023-09-07 The Katholieke Universiteit Leuven Tetrahydropyrazolopyrimidines and Related Analogs for Inhibiting YAP/TAZ-TEAD
WO2024039210A1 (ko) 2022-08-17 2024-02-22 한국화학연구원 Cdk2 및/또는 cdk9의 억제 또는 분해용 화합물 및 이들의 의약 용도

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008133192A1 (ja) 2007-04-19 2008-11-06 Takeda Pharmaceutical Company Limited 縮合イミダゾール化合物およびその用途
US8389521B2 (en) 2007-04-24 2013-03-05 Ingenium Pharmaceuticals Gmbh Inhibitors of protein kinases
JP5566880B2 (ja) 2007-04-24 2014-08-06 インゲニウム ファーマシューティカルズ ジーエムビーエイチ プロテインキナーゼの阻害剤としての4,6−二置換アミノピリミジン誘導体
JP5379787B2 (ja) 2007-04-24 2013-12-25 インゲニウム ファーマシューティカルズ ジーエムビーエイチ プロテインキナーゼの阻害剤
ES2539518T3 (es) 2007-04-24 2015-07-01 Astrazeneca Ab Inhibidores de proteínas quinasas
WO2008132138A1 (en) 2007-04-25 2008-11-06 Ingenium Pharmaceuticals Gmbh Derivatives of 4,6-disubstituted aminopyrimidines
EP2212297B1 (en) 2007-10-12 2011-05-25 Ingenium Pharmaceuticals GmbH Inhibitors of protein kinases
US20120157433A1 (en) 2009-09-04 2012-06-21 Pfister Keith B Heteroaryl Compounds as Kinase Inhibitors
US20110113038A1 (en) 2009-11-12 2011-05-12 International Business Machines Corporation Search term security
GB201002911D0 (en) 2010-02-19 2010-04-07 Medical Res Council Compound
AU2011226073B2 (en) 2010-03-10 2015-05-28 Astrazeneca Ab 4-Phenyl pyridine analogues as protein kinase inhibitors.
AR081810A1 (es) 2010-04-07 2012-10-24 Bayer Cropscience Ag Piridinilpirazoles biciclicos
WO2012066065A1 (en) 2010-11-17 2012-05-24 Novartis Ag Phenyl-heteroaryl amine compounds and their uses
WO2012101063A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyridine biaryl compounds and their uses
WO2012101064A1 (en) * 2011-01-28 2012-08-02 Novartis Ag N-acyl pyrimidine biaryl compounds as protein kinase inhibitors
EP2668162A1 (en) * 2011-01-28 2013-12-04 Novartis AG Substituted bi-heteroaryl compounds as cdk9 inhibitors and their uses
KR20140072177A (ko) 2011-10-06 2014-06-12 바이엘 인텔렉쳐 프로퍼티 게엠베하 헤테로사이클릴피리(미)디닐피라졸
CN105026393A (zh) 2013-03-13 2015-11-04 艾伯维公司 Cdk9激酶抑制剂
JP2016516710A (ja) 2013-03-13 2016-06-09 アッヴィ・インコーポレイテッド ピリジン系cdk9キナーゼ阻害薬
WO2014160028A1 (en) 2013-03-14 2014-10-02 Abbvie Inc. Pyrrolopyrimindine cdk9 kinase inhibitors
TW201446763A (zh) 2013-03-14 2014-12-16 Abbvie Inc 吡咯并[2,3-b]吡啶cdk9激酶抑制劑

Also Published As

Publication number Publication date
US20180093998A1 (en) 2018-04-05
SI3313838T1 (sl) 2019-06-28
JP6997627B2 (ja) 2022-01-17
MX2017016244A (es) 2018-04-20
EA201890094A1 (ru) 2018-07-31
PL3313838T3 (pl) 2019-08-30
TW201718573A (zh) 2017-06-01
HRP20190748T1 (hr) 2019-06-14
PT3539961T (pt) 2021-12-20
DK3313838T3 (da) 2019-06-11
CR20210297A (es) 2021-09-29
BR112017027394A2 (pt) 2018-11-06
AR105179A1 (es) 2017-09-13
US11352369B2 (en) 2022-06-07
DK3539961T3 (da) 2022-01-03
DOP2017000295A (es) 2017-12-31
CA2989499C (en) 2023-10-31
EP3539961B1 (en) 2021-10-06
CY1122111T1 (el) 2020-11-25
US9845331B2 (en) 2017-12-19
LT3539961T (lt) 2021-12-27
CN107873028B (zh) 2021-02-02
ZA201800563B (en) 2022-08-31
SV2017005598A (es) 2018-02-23
PH12017502334A1 (en) 2018-06-25
BR122019013677B1 (pt) 2024-01-02
EP3313838B1 (en) 2019-04-03
HUE057343T2 (hu) 2022-05-28
CR20170596A (es) 2018-07-04
CL2017003306A1 (es) 2018-06-29
DOP2018000207A (es) 2018-10-15
KR20180021830A (ko) 2018-03-05
ES2728356T3 (es) 2019-10-23
WO2017001354A1 (en) 2017-01-05
CY1125066T1 (el) 2023-03-24
US20210171541A1 (en) 2021-06-10
PT3313838T (pt) 2019-06-24
IL256393A (en) 2018-02-28
TWI723028B (zh) 2021-04-01
AU2016286200A1 (en) 2018-02-08
CN107873028A (zh) 2018-04-03
JP2018522869A (ja) 2018-08-16
LT3313838T (lt) 2019-06-10
RS62781B1 (sr) 2022-01-31
HRP20211970T1 (hr) 2022-03-18
US20160376287A1 (en) 2016-12-29
HUE043440T2 (hu) 2019-08-28
CO2017013713A2 (es) 2018-03-28
ME03404B (me) 2020-01-20
TN2017000486A1 (en) 2019-04-12
US10717746B2 (en) 2020-07-21
CA2989499A1 (en) 2017-01-05
PL3539961T3 (pl) 2022-02-14
EA035383B1 (ru) 2020-06-04
EP3313838A1 (en) 2018-05-02
IL256393B (en) 2021-12-01
RS58712B1 (sr) 2019-06-28
AU2016286200B2 (en) 2018-10-04
US20220340592A1 (en) 2022-10-27
MX371034B (es) 2020-01-13
ES2902148T3 (es) 2022-03-25
TR201909286T4 (tr) 2019-07-22
EP3539961A1 (en) 2019-09-18
NI201700174A (es) 2018-10-19
SI3539961T1 (sl) 2022-02-28

Similar Documents

Publication Publication Date Title
PE20180530A1 (es) Derivados de amidas policiclicas como inhibidores de cdk9
PE20161066A1 (es) Derivados de piperidinil-indol como inhibidores del factor de complemento b y usos de los mismos
EA201692095A1 (ru) Имидазо[4,5-c]хинолин-2-оновые соединения и их применение в лечении рака
MD4800C1 (ro) Compuşi de aminopirimidinil ca inhibitori de JAK
CL2017001422A1 (es) Pirazolo [1,5-a] pirazinas 4,6-sustituidas como inhibidores de janus cinasas
NZ749437A (en) Processes and intermediates for making a jak inhibitor
AR104326A1 (es) Compuestos nucleósidos 5-sustituidos
PH12015502047A1 (en) Novel pyrimidine and pyridine compounds and their usage
EA201592082A1 (ru) 3,4-дигидроизохинолин-2(1h)-ильные соединения
PH12015502502A1 (en) Heteroaromatic compounds and their use as dopamine d1 ligands
PE20170384A1 (es) Compuesto piridinicos de planieolida y metodos de uso
NZ624068A (en) Fused tricyclic compounds as raf kinase inhibitors
PE20190337A1 (es) NUEVOS DERIVADOS DE PIRROLO [2,3-d]PIRIMIDA, UN PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
PE20110549A1 (es) EL COMPUESTO 3-(4-CLORO-2-FLUOROBENCIL)-2-METIL-N-(5-METIL-1H-PIRAZOL-3-IL)-8-(MORFOLINOMETIL)IMIDAZO[1,2-b]PIRIDAZIN-6-AMINA, SUS SALES Y LA COMPOSICION QUE LO COMPRENDE
UA112795C2 (uk) Біциклічні піразинонові похідні
CY1122514T1 (el) Σουλφονικος υδροξυαιθυλεστερας του αναστολεα της εξαρτωμενης απο κυκλινη πρωτεϊνικης κινασης, κρυσταλλικη μορφη αυτου και μεθοδος παρασκευης αυτου
PE20180279A1 (es) Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak
NZ726790A (en) 1, 3, 4-thiadiazole compounds and their use in treating cancer
AR099071A1 (es) Antagonistas selectivos de nr2b
EA201791881A1 (ru) Производные 2-аминопиридина в качестве антагонистов рецептора аденозина aи лигандов рецепторов мелатонина mt
MX356759B (es) Derivados de pirimidinona como agentes antimalaricos.
CO2019002171A2 (es) Compuestos 8-(azetidín-1-il)-[1,2,4]triazolo[1,5-a]piridinilo, composiciones y métodos de utilización de los mismos.
AR106830A1 (es) Usos de piridazinonas para tratar el cáncer
TH127249B (th) สารประกอบเฮเทโรไซคลิค, การเตรียมของมัน และการใช้ของมันเชิงรักษา
AR103065A1 (es) Compuestos moduladores de fxr (nr1h4) que contiene grupos hidroxi