AR132802A1 - 2-amino-3-cianotiofenos con anillos espirocíclicos y derivados para el tratamiento del cáncer - Google Patents

2-amino-3-cianotiofenos con anillos espirocíclicos y derivados para el tratamiento del cáncer

Info

Publication number
AR132802A1
AR132802A1 ARP240101354A ARP240101354A AR132802A1 AR 132802 A1 AR132802 A1 AR 132802A1 AR P240101354 A ARP240101354 A AR P240101354A AR P240101354 A ARP240101354 A AR P240101354A AR 132802 A1 AR132802 A1 AR 132802A1
Authority
AR
Argentina
Prior art keywords
treatment
cyanothiophenes
cancer
derivatives
amino
Prior art date
Application number
ARP240101354A
Other languages
English (en)
Inventor
Joachim Broeker
Jason Abbott
Jianwen Cui
Stephen W Fesik
Andreas Gollner
Lorenz Herdeis
Tim Hodges
Andrew Little
Andreas Mantoulidis
Juergen Ramharter
Dhruba Sarkar
Kevin Sokol
Alex Waterson
Tobias Wunberg
Original Assignee
Boehringer Ingelheim Int
Univ Vanderbilt
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 Boehringer Ingelheim Int, Univ Vanderbilt filed Critical Boehringer Ingelheim Int
Publication of AR132802A1 publication Critical patent/AR132802A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente invención abarca compuestos de fórmula (1), donde R¹ᵃ, R¹ᵇ, R²ᵃ, R²ᵇ, Z, R³ a R⁵, el anillo A, el anillo B, p, q, V y W tienen los significados que se da en las reivindicaciones y en la memoria descriptiva, su uso como inhibidores de KRAS, composiciones farmacéuticas y preparaciones que contienen dichos compuestos y su uso como medicamentos / usos médicos, en especial como agentes para el tratamiento y/o la prevención de enfermedades oncológicas.
ARP240101354A 2023-05-30 2024-05-29 2-amino-3-cianotiofenos con anillos espirocíclicos y derivados para el tratamiento del cáncer AR132802A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP23175999 2023-05-30
EP23175994 2023-05-30

Publications (1)

Publication Number Publication Date
AR132802A1 true AR132802A1 (es) 2025-07-30

Family

ID=91375721

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP240101354A AR132802A1 (es) 2023-05-30 2024-05-29 2-amino-3-cianotiofenos con anillos espirocíclicos y derivados para el tratamiento del cáncer

Country Status (6)

Country Link
US (1) US20250019385A1 (es)
EP (1) EP4719603A1 (es)
CN (1) CN121487954A (es)
AR (1) AR132802A1 (es)
TW (1) TW202511268A (es)
WO (1) WO2024246099A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2024337913A1 (en) 2023-09-08 2026-03-26 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
WO2025190342A1 (zh) * 2024-03-15 2025-09-18 苏州浦合医药科技有限公司 螺环化合物作为kras突变体抑制剂
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025261393A1 (en) * 2024-06-19 2025-12-26 Insilico Medicine Ip Limited Novel compounds as kras inhibitors and uses thereof
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ592151A (en) 2008-12-12 2012-10-26 Boehringer Ingelheim Int Anti-igf antibodies
AR090151A1 (es) 2012-03-07 2014-10-22 Lilly Co Eli Compuestos inhibidores de raf
KR20140138910A (ko) 2012-03-14 2014-12-04 루핀 리미티드 헤테로사이클릴 화합물
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
JP6577958B2 (ja) 2014-04-11 2019-09-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング スピロ［３Ｈ−インドール−３，２’−ピロリジン］−２（１Ｈ）−オン誘導体およびＭＤＭ２−ｐ５３阻害剤としてのそれらの使用
JP6503386B2 (ja) 2014-07-03 2019-04-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＭＤＭ２−ｐ５３阻害剤としての新しいスピロ［３Ｈ−インドール−３，２’−ピロリジン］−２（１Ｈ）−オン化合物および誘導体
CA2956129C (en) 2014-08-21 2022-10-25 Boehringer Ingelheim International Gmbh New spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors
PL3359542T3 (pl) 2015-10-09 2021-09-20 Boehringer Ingelheim International Gmbh Związki i pochodne spiro[3h-indolo-3,2’-pirolidyno]-2(1h)-onowe jako inhibitory mdm2-p53
JP7219218B2 (ja) 2016-12-22 2023-02-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規のベンジルアミノ置換キナゾリンおよびｓｏｓ１阻害剤としての誘導体
CA3056970A1 (en) 2017-03-21 2018-09-27 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
WO2018204532A1 (en) 2017-05-03 2018-11-08 Vivace Therapeutics, Inc. Non-fused tricyclic compounds
RS64167B1 (sr) 2017-12-21 2023-05-31 Boehringer Ingelheim Int Benzilamino supstituisani piridopirimidinoni i derivati kao sos1 inhibitori
CA3097231A1 (en) 2018-04-18 2019-10-24 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
WO2020243423A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
PY2121402A (es) 2020-03-16 2022-08-09 Norvatis Ag Derivados de biarilo como inhibidores de la interacción proteína-proteína de yap/taz-tead
WO2021245055A1 (en) * 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CN118647620A (zh) * 2021-12-01 2024-09-13 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及其衍生物
US20250129096A1 (en) * 2021-12-01 2025-04-24 Boehringer Ingelheim Int'l GmbH Corp. Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099624A1 (en) * 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
JP2024543982A (ja) * 2021-12-01 2024-11-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング がんの処置のための縮環２－アミノ－３－シアノチオフェン及び誘導体
EP4452975A1 (en) 2021-12-23 2024-10-30 Boehringer Ingelheim International GmbH 8-aza quinazolines as brain-penetrant sos1-inhibitors

Also Published As

Publication number Publication date
WO2024246099A1 (en) 2024-12-05
EP4719603A1 (en) 2026-04-08
CN121487954A (zh) 2026-02-06
US20250019385A1 (en) 2025-01-16
TW202511268A (zh) 2025-03-16

Similar Documents

Publication Publication Date Title
AR132802A1 (es) 2-amino-3-cianotiofenos con anillos espirocíclicos y derivados para el tratamiento del cáncer
DOP2024000101A (es) Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cáncer
DOP2022000266A (es) 2-amino-3-cianotiofenos anulados y derivados para el tratamiento del cáncer
CL2021000907A1 (es) Nuevas piridopirimidinonas sustituidas con bencilamino y derivados como inhibidores de sos1 (divisional de solicitud n° 01501-2020)
CO2022015054A2 (es) [1,3]diazino[5,4-d]pirimidinas como inhibidores de her2
UY39786A (es) Derivados de Triazolopirimidina y su uso en el Tratamiento de Enfermedades
CL2022000271A1 (es) Inhibidores de la fosfatasa shp2 de pirazolo(3,4-b)pirazina.
CO2023005342A2 (es) Derivados de 1,2,3,4-tetrahidroquinolina como inhibidores de la activacion de yap/taz-tead para el tratamiento del cancer
MX2019010354A (es) Derivado de heteroaril[4,3-c]pirimidina-5-amina, metodo de preparacion del mismo y usos medicos del mismo.
DOP2021000198A (es) Compuestos y su uso en el tratamiento del cáncer
ECSP109935A (es) Derivados de morfolino pirimidina utilizados en enfermedades relacionadas con mtor quinasa y/o pi3k
UY38228A (es) Compuestos de triazolopirimidina y su uso en el tratamiento del cáncer
CO2022000749A2 (es) Inhibidores de monoacilglicerol lipasa (magl) heterocíclicos
MX2024006975A (es) Inhibidor de cdk9 y uso del mismo.
ECSP19026973A (es) Derivados de naftiridinona y su uso en el tratamiento de la arritmia
ECSP22083772A (es) Compuestos y composiciones para inhibir la actividad de hif2-alfa y sus métodos de uso
CL2025002997A1 (es) Derivados bicíclicos semisaturados y usos relacionados.
CO2024014215A2 (es) Formulaciones de inhibidor de tyk2 y métodos para elaborarlas
AR131001A1 (es) Inhibidores de la proteína tirosina fosfatasa, composiciones y métodos de uso
CL2023003209A1 (es) Composición farmacéutica de pembrolizumab y su uso
ECSP24050199A (es) Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cáncer
CO2020012484A2 (es) Inhibidores de secreción de proteínas basados en triazaciclododecansulfonamida ("tcd")
CO2025001849A2 (es) Compuestos de imidazopiridina, preparación de los mismos y usos terapéuticos de los mismos
AR134062A1 (es) Inhibidores de ras y sus métodos de uso
AR131249A1 (es) Derivados de heteroarilo bicíclicos útiles como agentes anticancerígenos

Legal Events

Date Code Title Description
FB Suspension of granting procedure