PE20211868A1 - Derivados de 2,3-dihidro-1h-pirrolo[3,4-c]piridin-1-ona como inhibidores de hpk1 para el tratamiento del cancer - Google Patents

Derivados de 2,3-dihidro-1h-pirrolo[3,4-c]piridin-1-ona como inhibidores de hpk1 para el tratamiento del cancer

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Publication number
PE20211868A1
PE20211868A1 PE2021000685A PE2021000685A PE20211868A1 PE 20211868 A1 PE20211868 A1 PE 20211868A1 PE 2021000685 A PE2021000685 A PE 2021000685A PE 2021000685 A PE2021000685 A PE 2021000685A PE 20211868 A1 PE20211868 A1 PE 20211868A1
Authority
PE
Peru
Prior art keywords
pyridin
dihydro
halogen
alkyl
methyl
Prior art date
Application number
PE2021000685A
Other languages
English (en)
Inventor
Rebecca Anne Gallego
Sajiv Krishnan Nair
Robert Steven Kania
Omar Khaled Ahmad
Ted William Johnson
Jamison Bryce Tuttle
Mehran Jalaie
Michele Ann Mctigue
Dahui Zhou
Bel Matthew L Del
Ru Zhou
Mingying He
Anne-Marie Dechert Schmitt
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of PE20211868A1 publication Critical patent/PE20211868A1/es

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    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Esta referido a un derivado de 2,3-dihidro-1H-pirrolo[3,4-c]piridin-1-ona de Formula I, en donde: R1 es H, halogeno, alquilo, haloalquilo, entre otros; R1a es H, halogeno; R2 es -(CH2)mN(R8)(R9), alquilo, heterocicloalquilo; R3 es H, halogeno, hidroxi, alquilo, entre otros; R4 es heterocicloalquilo o heteroarilo; R5 es H, halogeno, OH; alquilo, entre otros; a es 0, 1. Entre los compuestos preferidos tenemos los siguientes: 4-[(metilamino)metil]-6-[metil(propan-2-il)amino]-2-[6-(4-propil-4H-1,2,4-triazol3-il)piridin-2-il]-2,3-dihidro-1H-pirrolo[3,4-c]piridin-1-ona; 4-[(metilamino)metil]-2-[6-(5-metil-4-propil-4H-1,2,4-triazol-3-il)piridin-2-il]-6- [(2R)-2-metilpirrolidin-1-il]-2,3-dihidro-1H-pirrolo[3,4-c]piridin-1-ona; entre otros. Estos compuestos son inhibidores de hematopoyetica progenitora quinasa 1 (HPK1) y son utiles para tratar o mejorar trastornos proliferativos celulares anormales, tales como cancer.
PE2021000685A 2018-11-15 2019-11-12 Derivados de 2,3-dihidro-1h-pirrolo[3,4-c]piridin-1-ona como inhibidores de hpk1 para el tratamiento del cancer PE20211868A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862767602P 2018-11-15 2018-11-15
US201962909970P 2019-10-03 2019-10-03
PCT/IB2019/059702 WO2020100027A1 (en) 2018-11-15 2019-11-12 2,3-dihydro-1h-pyrrolo[3,4-c]pyridin-1-one derivatives as hpk1 inhibitors for the treatment of cancer

Publications (1)

Publication Number Publication Date
PE20211868A1 true PE20211868A1 (es) 2021-09-21

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Country Status (36)

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US (1) US11142525B2 (es)
EP (1) EP3880676B1 (es)
JP (1) JP7118267B2 (es)
KR (1) KR20210090675A (es)
CN (1) CN113316576A (es)
AU (1) AU2019378184B2 (es)
BR (1) BR112021008991A2 (es)
CA (1) CA3061392A1 (es)
CL (1) CL2021001190A1 (es)
CO (1) CO2021006114A2 (es)
CR (1) CR20210251A (es)
CU (1) CU20210035A7 (es)
DK (1) DK3880676T3 (es)
DO (1) DOP2021000088A (es)
EC (1) ECSP21034668A (es)
ES (1) ES2958948T3 (es)
FI (1) FI3880676T3 (es)
GE (1) GEP20227434B (es)
HR (1) HRP20231089T1 (es)
HU (1) HUE063367T2 (es)
IL (1) IL283149A (es)
LT (1) LT3880676T (es)
MD (1) MD3880676T2 (es)
MX (1) MX2021005754A (es)
PE (1) PE20211868A1 (es)
PH (1) PH12021551117A1 (es)
PL (1) PL3880676T3 (es)
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RS (1) RS64655B1 (es)
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SI (1) SI3880676T1 (es)
TW (1) TWI718758B (es)
UA (1) UA127426C2 (es)
UY (1) UY38471A (es)
WO (1) WO2020100027A1 (es)
ZA (1) ZA202103099B (es)

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PE20211655A1 (es) 2018-10-31 2021-08-24 Gilead Sciences Inc Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1
TWI721624B (zh) 2018-10-31 2021-03-11 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
TWI826690B (zh) 2019-05-23 2023-12-21 美商基利科學股份有限公司 經取代之烯吲哚酮化物及其用途
CA3181415A1 (en) * 2020-05-01 2021-11-04 Pfizer Inc. Azalactam compounds as hpk1 inhibitors
CN112409268A (zh) * 2020-12-03 2021-02-26 西南交通大学 靶向Fam20C抑制剂的制备及其抗三阴性乳腺癌作用
CN117460732A (zh) * 2021-06-11 2024-01-26 杭州中美华东制药有限公司 吡咯并吡啶酮类化合物及其制备方法和用途
TW202321239A (zh) 2021-07-20 2023-06-01 瑞典商阿斯特捷利康公司 作為hpk1抑制劑用於治療癌症之經取代的吡𠯤—2—甲醯胺
WO2023023942A1 (en) * 2021-08-24 2023-03-02 Biofront Ltd (Cayman) Hpk1 inhibitors, compositions comprising hpk1 inhibitor, and methods of using the same
CN118103369A (zh) * 2021-09-03 2024-05-28 浙江海正药业股份有限公司 吡啶并内酰胺类衍生物及其制备方法和用途
WO2023057883A1 (en) * 2021-10-05 2023-04-13 Pfizer Inc. Crystalline form of azalactam compound

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KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
US5243049A (en) * 1992-01-22 1993-09-07 Neurogen Corporation Certain pyrroloquinolinones: a new class of GABA brain receptor ligands
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
BRPI0814441A2 (pt) * 2007-07-19 2015-07-14 Schering Corp Compostos de amida heterocíclica como inibidores de proteína cinase
WO2018049324A1 (en) 2016-09-12 2018-03-15 Numerate, Inc. Monocyclic compounds useful as gpr120 modulators
JP7132937B2 (ja) 2017-03-15 2022-09-07 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト Hpk1の阻害剤としてのアザインドール
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Publication number Publication date
FI3880676T3 (fi) 2023-09-15
ZA202103099B (en) 2023-11-29
CU20210035A7 (es) 2021-12-08
CL2021001190A1 (es) 2021-12-24
US11142525B2 (en) 2021-10-12
CN113316576A (zh) 2021-08-27
PT3880676T (pt) 2023-10-04
UY38471A (es) 2020-06-30
UA127426C2 (uk) 2023-08-16
MX2021005754A (es) 2021-08-11
TWI718758B (zh) 2021-02-11
US20200172539A1 (en) 2020-06-04
MD3880676T2 (ro) 2023-12-31
AU2019378184B2 (en) 2022-09-15
ES2958948T3 (es) 2024-02-16
TW202031657A (zh) 2020-09-01
DOP2021000088A (es) 2021-06-30
JP2022507231A (ja) 2022-01-18
HRP20231089T1 (hr) 2023-12-22
SG11202104394XA (en) 2021-05-28
PL3880676T3 (pl) 2023-12-11
EP3880676A1 (en) 2021-09-22
CR20210251A (es) 2021-07-14
AU2019378184A1 (en) 2021-05-27
DK3880676T3 (da) 2023-09-04
CA3061392A1 (en) 2020-05-15
KR20210090675A (ko) 2021-07-20
SI3880676T1 (sl) 2023-10-30
IL283149A (en) 2021-06-30
EP3880676B1 (en) 2023-08-02
HUE063367T2 (hu) 2024-01-28
GEP20227434B (en) 2022-10-25
RS64655B1 (sr) 2023-10-31
BR112021008991A2 (pt) 2021-08-10
CO2021006114A2 (es) 2021-05-31
PH12021551117A1 (en) 2021-11-22
WO2020100027A1 (en) 2020-05-22
LT3880676T (lt) 2023-09-25
JP7118267B2 (ja) 2022-08-15
ECSP21034668A (es) 2021-06-30

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