PE20230824A1 - Inhibidores alostericos de cromenona del fosfoinositido 3-quinasa (pi3k) para el tratamiento de enfermedades - Google Patents

Inhibidores alostericos de cromenona del fosfoinositido 3-quinasa (pi3k) para el tratamiento de enfermedades

Info

Publication number
PE20230824A1
PE20230824A1 PE2022002162A PE2022002162A PE20230824A1 PE 20230824 A1 PE20230824 A1 PE 20230824A1 PE 2022002162 A PE2022002162 A PE 2022002162A PE 2022002162 A PE2022002162 A PE 2022002162A PE 20230824 A1 PE20230824 A1 PE 20230824A1
Authority
PE
Peru
Prior art keywords
cancer
phosphoinositide
pi3k
kinase
allosteric inhibitors
Prior art date
Application number
PE2022002162A
Other languages
English (en)
Inventor
Erin Danielle Anderson
Sean Douglas Aronow
Nicholas A Boyles
Markus K Dahlgren
Shulu Feng
Aleksey I Gerasyuto
Eugene R Hickey
Thomas Combs Irvin
Edward A Kesicki
Anke Klippel-Giese
Jennifer Lynn Knight
Gabrielle R Kolakowski
Manoj Kumar
Katelyn Frances Long
Christopher Glenn Mayne
David L Mcelligott
Johnathan Alexander; Mclean
Loredana Puca
Kannan Karukurichi Ravi
Daniel Lee Severance
Michael Brian Welch
Tien Widjaja
Original Assignee
Petra Pharma Corp
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 Petra Pharma Corp filed Critical Petra Pharma Corp
Publication of PE20230824A1 publication Critical patent/PE20230824A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Referido a un compuesto de formula (I), o un profarmaco, solvato, enantiomero, estereoisomero, tautomero o sal farmaceuticamente aceptable de este, en donde: X es -NR12- o -O-; Y es -C(R11)2-, -O-, -NR11- o -S-; cada R3, R4, R5 y R6 es independientemente H, halogeno, -CN, alquilo C1-C6, entre otros; cada R7 y R8 es independientemente H, halogeno, -CN, alquilo C1-C6, entre otros; al menos un R9 es -C(O)OR12; el Anillo A es cicloalquilo C3-C10, arilo, heterociclo que comprende 1-4 heteroatomos seleccionados de N, O y S, entre otros; y s es 1, 2, 3, 4, 5 o 6. Un compuesto seleccionado es acido (2-((1-(2-(4,4-dimetilpiperidin-1-il)-6-metil-4-oxo-4H-cromen-8-il)etil)amino)fenil)boronico. Dichos compuestos son inhibidores alostericos de cromenona del fosfoinositido 3-quinasa (PI3K). Tambien refiere a una composicion farmaceutica siendo utiles para tratar una enfermedad o un trastorno asociado con la modulacion de la fosfoinositido 3-quinasa (PI3K), tal como el cancer, en particular cancer de endometrio, cancer gastrico, leucemia, linfoma, sarcoma, cancer colorrectal, cancer de pulmon, cancer de ovario, entre otros.
PE2022002162A 2020-04-03 2021-04-02 Inhibidores alostericos de cromenona del fosfoinositido 3-quinasa (pi3k) para el tratamiento de enfermedades PE20230824A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063005096P 2020-04-03 2020-04-03
PCT/US2021/025521 WO2021202964A1 (en) 2020-04-03 2021-04-02 Allosteric chromenone inhibitors of phosphoinositide 3-kinase (pi3k) for the treatment of diseases associated with p13k modulation

Publications (1)

Publication Number Publication Date
PE20230824A1 true PE20230824A1 (es) 2023-05-19

Family

ID=75674963

Family Applications (1)

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PE2022002162A PE20230824A1 (es) 2020-04-03 2021-04-02 Inhibidores alostericos de cromenona del fosfoinositido 3-quinasa (pi3k) para el tratamiento de enfermedades

Country Status (18)

Country Link
US (2) US11649227B2 (es)
EP (1) EP4126851A1 (es)
JP (1) JP7505023B2 (es)
KR (1) KR20220163462A (es)
CN (1) CN115956075A (es)
AR (1) AR121719A1 (es)
AU (1) AU2021248415B2 (es)
BR (1) BR112022019918A2 (es)
CA (1) CA3173569A1 (es)
CO (1) CO2022014160A2 (es)
CR (1) CR20220493A (es)
EC (1) ECSP22077299A (es)
IL (1) IL296918A (es)
JO (1) JOP20220247A1 (es)
MX (1) MX2022012306A (es)
PE (1) PE20230824A1 (es)
TW (1) TWI794780B (es)
WO (1) WO2021202964A1 (es)

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AR121719A1 (es) * 2020-04-03 2022-06-29 Petra Pharma Corp Inhibidores alostéricos de cromenona del fosfoinosítido 3-quinasa (pi3k) para el tratamiento de enfermedades
CR20230517A (es) 2021-05-03 2023-11-28 Petra Pharma Corp Inhibidores alostéricos de cromenona del fosfoinosítido 3-quinasa (pi3k) para el tratamiento de enfermedades
TWI829179B (zh) 2021-05-27 2024-01-11 美商佩特拉製藥公司 用於治療疾病之磷酸肌醇3-激酶(pi3k)異位色烯酮抑制劑
TW202334137A (zh) * 2021-11-03 2023-09-01 美商薩諾管理公司 Pi3k抑制劑及治療癌症之方法
WO2023104111A1 (en) * 2021-12-08 2023-06-15 Nanjing Zenshine Pharmaceuticals Co., Ltd. Fused heterocyclic compounds as pi3kalpha inhibitors
AU2022421224A1 (en) * 2021-12-22 2024-06-20 The Regents Of The University Of California Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase
US20240124422A1 (en) * 2022-03-29 2024-04-18 Prelude Therapeutics Incorporated Mutant pi3k-alpha inhibitors and their use as pharmaceuticals
TW202404968A (zh) * 2022-04-20 2024-02-01 美商思諾維新醫藥公司 PI3Kα抑制劑
WO2023207881A1 (en) * 2022-04-24 2023-11-02 InventisBio Co., Ltd. Compounds, preparation methods and uses thereof
TW202408481A (zh) * 2022-04-29 2024-03-01 美商佩特拉製藥公司 用於治療疾病之磷酸肌醇3-激酶(pi3k)異位色烯酮抑制劑
WO2023239710A1 (en) 2022-06-08 2023-12-14 Onkure, Inc. Benzopyrimidin-4(3h)-ones as pi3k inhibitors
CN117362281A (zh) * 2022-07-07 2024-01-09 海创药业股份有限公司 一种pi3k抑制剂及其制备方法和用途
WO2024054469A1 (en) 2022-09-08 2024-03-14 Onkure, Inc. Isoquinolones as pi3k inhibitors
WO2024051778A1 (en) * 2022-09-09 2024-03-14 InventisBio Co., Ltd. Compounds, preparation methods and uses thereof
WO2024064024A1 (en) 2022-09-19 2024-03-28 Onkure, Inc. ((4-oxo-3,4-dihydroquinazolin-8-yl)methyl)amine derivatives as p13k inhibitors for the treatment of cancer
WO2024081345A1 (en) 2022-10-14 2024-04-18 Onkure, Inc. Benzopyrimidin-4(3h)-ones as pi3k inhibitors
WO2024081904A1 (en) * 2022-10-14 2024-04-18 Genesis Therapeutics, Inc. Methods for treating cancer
US20240182460A1 (en) * 2022-11-01 2024-06-06 Petra Pharma Corporation Allosteric chromenone inhibitors of phosphoinositide 3-kinase (pi3k) for the treatment of disease
WO2024097205A1 (en) * 2022-11-02 2024-05-10 Petra Pharma Corporation Allosteric chromenone inhibitors of phosphoinositide 3-kinase (pi3k) for the treatment of disease
WO2024097721A1 (en) 2022-11-02 2024-05-10 Petra Pharma Corporation Targeting allosteric and orthosteric pockets of phosphoinositide 3-kinase (pi3k) for the treatment of disease
WO2024099437A1 (en) * 2022-11-11 2024-05-16 Fochon Biosciences, Ltd. Compounds as protein kinase inhibitors

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TW202200567A (zh) 2022-01-01
US11649227B2 (en) 2023-05-16
AR121719A1 (es) 2022-06-29
AU2021248415B2 (en) 2024-03-21
AU2021248415A1 (en) 2022-10-20
CR20220493A (es) 2022-12-15
MX2022012306A (es) 2023-01-04
IL296918A (en) 2022-12-01
US20220372023A1 (en) 2022-11-24
JOP20220247A1 (ar) 2023-01-30
TWI794780B (zh) 2023-03-01
US20230286960A1 (en) 2023-09-14
JP2023521321A (ja) 2023-05-24
CN115956075A (zh) 2023-04-11
BR112022019918A2 (pt) 2023-02-14
WO2021202964A1 (en) 2021-10-07
CO2022014160A2 (es) 2023-02-16
KR20220163462A (ko) 2022-12-09
JP7505023B2 (ja) 2024-06-24
ECSP22077299A (es) 2023-01-31
EP4126851A1 (en) 2023-02-08
CA3173569A1 (en) 2021-10-07

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