PE20220704A1 - Derivados de 3,6-diamino-piridazin-3-ilo, composiciones farmaceuticas que los contienen y sus usos como agentes proapoptoticos - Google Patents

Derivados de 3,6-diamino-piridazin-3-ilo, composiciones farmaceuticas que los contienen y sus usos como agentes proapoptoticos

Info

Publication number
PE20220704A1
PE20220704A1 PE2022000148A PE2022000148A PE20220704A1 PE 20220704 A1 PE20220704 A1 PE 20220704A1 PE 2022000148 A PE2022000148 A PE 2022000148A PE 2022000148 A PE2022000148 A PE 2022000148A PE 20220704 A1 PE20220704 A1 PE 20220704A1
Authority
PE
Peru
Prior art keywords
compound
pyridazin
diamino
proapoptotic agents
derivatives
Prior art date
Application number
PE2022000148A
Other languages
English (en)
Inventor
James Edward Paul Davidson
Tibor Novak
Attila Paczal
Andras Kotschy
Jerôme-Benoît Starck
James Brooke Murray
Simon Bedford
Maia Chanrion
Frederic Colland
Patrice Desos
Mark Philip Dodsworth
Petra Dunkel
Andras Herner
Zoltan Madarasz
Ana Leticia Maragno
Mark Molnar
Miklos Nyerges
Rachel Jane Parsons
Monika Rudasova
Agnes Strofek
Marianna Szigeti
Matyas Pal Timari
Paul Webb
Original Assignee
Servier Lab
Vernalis Randd Ltd
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 Servier Lab, Vernalis Randd Ltd filed Critical Servier Lab
Publication of PE20220704A1 publication Critical patent/PE20220704A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/502Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • 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)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Referido a un compuesto de formula (I) en donde: R1 y R2, independientemente uno de otro, representan un grupo seleccionado de: H; alquiloC1-C6 lineal o ramificado sustituido opcionalmente con un grupo hidroxilo o un grupo alcoxiC1-C6, entre otros; R3 representa un grupo seleccionado de: hidrogeno; cicloalquiloC3-C6; alquiloC1-C6 lineal o ramificado, entre otros. Un compuesto seleccionado es Acido 2-({6-[(1,3-benzotiazol-2-il)amino]-5-metilpiridazin-3-il}(4-hidroxibutil)amino)-5-(3-{2-fluoro-4-[3-(metilamino)prop-1-in-1-il]fenoxi}propil)-1,3-tiazol-4-carboxilico. Estos compuestos derivados de 3,6-diamino-piridazin-3-ilo son agentes proapoptoticos, inhibidores potentes selectivos de Bcl-xL. Tambien se refiere a compuestos intermedios, metodo de preparacion de los mismos, a una composicion farmaceutica que comprende dicho compuesto, una sal de adicion del mismo con un acido o base farmaceuticamente aceptable en combinacion con uno o mas excipientes farmaceuticamente aceptables, y su uso en el tratamiento del cancer o enfermedades autoinmunes.
PE2022000148A 2019-07-29 2020-07-28 Derivados de 3,6-diamino-piridazin-3-ilo, composiciones farmaceuticas que los contienen y sus usos como agentes proapoptoticos PE20220704A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19188747 2019-07-29
PCT/EP2020/071179 WO2021018857A1 (en) 2019-07-29 2020-07-28 3,6-diamino-pyridazin-3-yl derivatives, pharmaceutical compositions containing them and their uses as pro-apoptotic agents

Publications (1)

Publication Number Publication Date
PE20220704A1 true PE20220704A1 (es) 2022-05-04

Family

ID=67514281

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000148A PE20220704A1 (es) 2019-07-29 2020-07-28 Derivados de 3,6-diamino-piridazin-3-ilo, composiciones farmaceuticas que los contienen y sus usos como agentes proapoptoticos

Country Status (19)

Country Link
US (1) US20220289734A1 (es)
EP (1) EP4003988A1 (es)
JP (1) JP2022542937A (es)
KR (1) KR20220042182A (es)
CN (1) CN114450283B (es)
AR (1) AR119493A1 (es)
AU (1) AU2020322072A1 (es)
BR (1) BR112022001330A2 (es)
CA (1) CA3148502A1 (es)
CL (1) CL2021003594A1 (es)
CO (1) CO2022000700A2 (es)
CR (1) CR20220014A (es)
IL (1) IL289932A (es)
JO (1) JOP20220006A1 (es)
MX (1) MX2022001161A (es)
PE (1) PE20220704A1 (es)
TW (1) TW202118761A (es)
UY (1) UY38809A (es)
WO (1) WO2021018857A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL303048A (en) * 2020-11-24 2023-07-01 Novartis Ag BCL-XL inhibitor antibody-drug conjugates and methods of using them
JP2024505562A (ja) * 2021-02-02 2024-02-06 レス ラボラトイレス セルビエル 選択的bcl-xl protac化合物及び使用の方法
TW202408588A (zh) 2022-05-20 2024-03-01 瑞士商諾華公司 抗體-藥物結合物抗腫瘤化合物及其使用方法
WO2023225336A1 (en) 2022-05-20 2023-11-23 Novartis Ag Met bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
WO2023225320A1 (en) 2022-05-20 2023-11-23 Novartis Ag Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006503796A (ja) * 2001-12-21 2006-02-02 バイエル・フアーマシユーチカルズ・コーポレーシヨン ピリダジンまたはピリジン誘導体を含んでなる抗−脈管形成組み合わせ療法
WO2009020603A2 (en) * 2007-08-08 2009-02-12 The Scripps Research Institute Upp amphiphilic alpha-helix mimetics
AU2008343932B2 (en) * 2007-12-19 2013-08-15 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
FR3015483B1 (fr) 2013-12-23 2016-01-01 Servier Lab Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2016194831A1 (ja) * 2015-05-29 2016-12-08 帝人ファーマ株式会社 ピリド[3,4-d]ピリミジン誘導体及びその薬学的に許容される塩

Also Published As

Publication number Publication date
CN114450283A (zh) 2022-05-06
CR20220014A (es) 2022-03-02
JOP20220006A1 (ar) 2023-01-30
MX2022001161A (es) 2022-02-22
CA3148502A1 (en) 2021-02-04
CN114450283B (zh) 2024-05-07
AR119493A1 (es) 2021-12-22
CO2022000700A2 (es) 2022-02-07
TW202118761A (zh) 2021-05-16
UY38809A (es) 2021-02-26
AU2020322072A1 (en) 2022-02-10
BR112022001330A2 (pt) 2022-05-17
US20220289734A1 (en) 2022-09-15
IL289932A (en) 2022-03-01
KR20220042182A (ko) 2022-04-04
EP4003988A1 (en) 2022-06-01
WO2021018857A1 (en) 2021-02-04
CL2021003594A1 (es) 2022-11-18
JP2022542937A (ja) 2022-10-07

Similar Documents

Publication Publication Date Title
PE20220704A1 (es) Derivados de 3,6-diamino-piridazin-3-ilo, composiciones farmaceuticas que los contienen y sus usos como agentes proapoptoticos
PE20220705A1 (es) Derivados de 6,7-dihidro-5h-pirido[2,3-c]piridazin y compuestos relacionados como inhibidores de proteina bcl-xl y agentes proapoptoticos para el tratamiento del cancer
PE20220931A1 (es) Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
PE20230249A1 (es) Compuestos de heteroarilo biciclicos y usos de estos
AR046297A1 (es) Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo
AR037534A1 (es) Derivado de adamantano, su uso en la fabricacion de un medicamento para usar en terapia, composicion farmaceutica, proceso para la preparacion de dicho compuesto y dicha composicion y compuestos intermediarios
PE20230239A1 (es) Derivado de arilamida con actividad antitumoral
AR065464A1 (es) Derivados de nicotinamida. composiciones farmaceuticas
PE20212303A1 (es) Inhibidores aza-heterobiciclicos de mat2a y metodos de uso en el tratamiento de cancer
PE20201256A1 (es) Compuestos monobactamicos cromanos para el tratamiento de infecciones bacterianas
AR056762A1 (es) (4 -(6-halo-7- substituidos -2,4- dioxo-1,4- dihidro-2h-quinazolin-3-il- fenil)-5- cloro- tiophen-2- il sulfonilureas y formas y metodos
AR057855A1 (es) Derivados de pirazina y composicion farmaceutica
AR056574A1 (es) Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso
AR058180A1 (es) Indeno derivados, su preparacion y su uso como medicamentos
AR074608A1 (es) Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas
AR066103A1 (es) Derivados de triazolopiridin - carboxamidas, su preparacion y su aplicacion en terapeutica
AR046085A1 (es) Agonistas etilamino amino sustituidos del receptor beta 2 adrenergico
PE20230235A1 (es) Compuestos para modular la actividad de fxr y usos de los mismos
AR062737A1 (es) Composicion farmaceutica que comprende un compuesto derivado de aril-azabiciclo, compuesto correspondiente y su uso para la preparacion de un medicamento
PE20200445A1 (es) Inhibidores pirazolicos de magl
PE20190964A1 (es) Inhibidores de dopamina-b-hidroxilasa penetrantes de la barrera hematoencefalica
PE20211769A1 (es) Compuestos heteroaromaticos como inhibidores de vanina
PE20220252A1 (es) Compuestos de pirrol
AR060064A1 (es) Compuestos sustituidos de tetrahidroisoquinolina, su preparacion y su uso en medicamentos para el tratamiento de enfermedades mediadas por los receptores 5-ht6