AR114419A1 - 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PREVENTION OF LIVER CANCER - Google Patents

7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PREVENTION OF LIVER CANCER

Info

Publication number
AR114419A1
AR114419A1 ARP190100505A ARP190100505A AR114419A1 AR 114419 A1 AR114419 A1 AR 114419A1 AR P190100505 A ARP190100505 A AR P190100505A AR P190100505 A ARP190100505 A AR P190100505A AR 114419 A1 AR114419 A1 AR 114419A1
Authority
AR
Argentina
Prior art keywords
alkyl
benzyl
amino
propylsulfonimidoyl
carbonyl
Prior art date
Application number
ARP190100505A
Other languages
Spanish (es)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR114419A1 publication Critical patent/AR114419A1/en

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
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/39—Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente se refiere a compuestos de fórmula (1), en donde R¹, R² y R³ son como se describen en el presente documento, y sus profármacos o sales farmacéuticamente aceptables, enantiómeros o diastereómeros de los mismos, para (su uso en) el tratamiento y/o profilaxis del cáncer de hígado. Reivindicación 1: Un compuesto de fórmula (1), donde R¹ es alquilo-C₁₋₆; R² es bencilo, estando dicho bencilo sin sustituir o sustituido con uno, dos o tres sustituyentes seleccionados independientemente entre halógeno y alquilo C₁₋₆; R³ es -NR⁴R⁵, en donde R⁴ es alquilo-C₁₋₆ o alcoxi-C₁₋₆-alquilo-C₁₋₆; R⁵ es (alquil-C₁₋₆)₂NCOO-alquilo-C₁₋₆, alcoxi-C₁₋₆-alquilo-C₁₋₆, alcoxi-C₁₋₆carbonil(alquil-C₁₋₆) aminoalquilo-C₁₋₆, alcoxi-C₁₋₆carbonil(fenil)alquilo-C₁₋₆, alcoxi-C₁₋₆carbonil-alquilo-C₁₋₆, alcoxi-C₁₋₆carboniloxi-alquilo-C₁₋₆, alquilo-C₁₋₆, alquil-C₁₋₆carbonil(alquil-C₁₋₆)aminoalquilo-C₁₋₆ o pirrolidinilcarbamoíloxialquilo-C₁₋₆; o R⁴ y R⁵ junto con el nitrógeno se unen para formar un heterociclilo; o una sal, enantiómero o diastereómero farmacéuticamente aceptable del mismo; para su uso en el tratamiento o profilaxis del cáncer de hígado; con la condición de que 6-amino-9-bencil-2-(propilsulfonimidoil)-7-(pirrolidina-1-carbonil)-purin-8-ona; 6-amino-9-bencilo-7-(piperidina-1-carbonil)-2-(propilsulfonimidoil)-purin-8-ona; 6-amino-9-bencil-7-(morfolina-4-carbonil)-2-(propilsulfonimidoil)-purin-8-ona; 6-amino-9-bencil-7-(3,3-dimetilpirrolidina-1-carbonil)-2-(propilsulfonimidoil)-purin-8-ona; 1-[6-amino-9-bencil-8-oxo-2-(propilsulfonimidoil)-purin-7-carbonil]pirrolidina-2-carboxilato de etilo; 6-amino-7-(2-azaspiro[3,3]heptano-2-carbonil)-9-bencil-2-(propilsulfonimidoil)-purin-8-ona; 6-amino-9-bencil-7-(2-oxa-6-azaspiro[3,3]heptano-6-carbonil)-2-(propilsulfonimidoil)-purin-8-ona; 6-amino-9-bencil-7-(3,3-difluoropirrolidina-1-carbonil)-2-(propilsulfonimidoil)-purin-8-ona; 6-amino-9-bencil-7-(3-fluoro-3-metil-pirrolidina-1-carbonil)-2-(propilsulfonimidoil)-purin-8-ona; y se excluyen sus enantiómeros o diastereómeros.The present refers to compounds of formula (1), wherein R¹, R² and R³ are as described herein, and their prodrugs or pharmaceutically acceptable salts, enantiomers or diastereomers thereof, for (use in) the treatment and / or prophylaxis of liver cancer. Claim 1: A compound of formula (1), wherein R¹ is C₁₋₆-alkyl; R² is benzyl, said benzyl being unsubstituted or substituted with one, two or three substituents independently selected from halogen and C₁₋₆ alkyl; R³ is -NR⁴R⁵, where R⁴ is C₁₋₆-alkyl or C₁₋₆-alkoxy-C₁₋₆-alkyl; R⁵ is (C₁₋₆-alkyl) ₂NCOO-C₁₋₆-alkyl, C₁₋₆-alkoxy-C₁₋₆-alkyl, C₁₋₆-alkoxycarbonyl (C₁₋₆-alkyl) amino-C₁₋₆-alkyl, C₁-alkoxy ₋₆carbonyl (phenyl) C₁₋₆-alkyl, C alco-alkoxycarbonyl-C₁₋₆-alkyl, C₁₋₆-alkoxycarbonyloxy-C₁₋₆-alkyl, C₁₋₆-alkyl, C₁₋₆-alkyl (C₁-alkyl *) C₁₋₆-aminoalkyl or C₁₋₆-pyrrolidinylcarbamoyloxyalkyl; or R⁴ and R⁵ together with the nitrogen join to form a heterocyclyl; or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof; for use in the treatment or prophylaxis of liver cancer; with the proviso that 6-amino-9-benzyl-2- (propylsulfonimidoyl) -7- (pyrrolidine-1-carbonyl) -purin-8-one; 6-amino-9-benzyl-7- (piperidine-1-carbonyl) -2- (propylsulfonimidoyl) -purin-8-one; 6-amino-9-benzyl-7- (morpholine-4-carbonyl) -2- (propylsulfonimidoyl) -purin-8-one; 6-amino-9-benzyl-7- (3,3-dimethylpyrrolidine-1-carbonyl) -2- (propylsulfonimidoyl) -purin-8-one; Ethyl 1- [6-amino-9-benzyl-8-oxo-2- (propylsulfonimidoyl) -purine-7-carbonyl] pyrrolidine-2-carboxylate; 6-amino-7- (2-azaspiro [3,3] heptane-2-carbonyl) -9-benzyl-2- (propylsulfonimidoyl) -purin-8-one; 6-amino-9-benzyl-7- (2-oxa-6-azaspiro [3,3] heptane-6-carbonyl) -2- (propylsulfonimidoyl) -purin-8-one; 6-amino-9-benzyl-7- (3,3-difluoropyrrolidine-1-carbonyl) -2- (propylsulfonimidoyl) -purin-8-one; 6-amino-9-benzyl-7- (3-fluoro-3-methyl-pyrrolidine-1-carbonyl) -2- (propylsulfonimidoyl) -purin-8-one; and their enantiomers or diastereomers are excluded.

ARP190100505A 2018-02-28 2019-02-28 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PREVENTION OF LIVER CANCER AR114419A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2018077501 2018-02-28

Publications (1)

Publication Number Publication Date
AR114419A1 true AR114419A1 (en) 2020-09-02

Family

ID=65685310

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP190100505A AR114419A1 (en) 2018-02-28 2019-02-28 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PREVENTION OF LIVER CANCER

Country Status (19)

Country Link
EP (1) EP3758707A1 (en)
JP (1) JP7089596B2 (en)
KR (1) KR20200128414A (en)
CN (1) CN111801100B (en)
AR (1) AR114419A1 (en)
AU (1) AU2019228654A1 (en)
BR (1) BR112020016509A2 (en)
CA (1) CA3091950A1 (en)
CL (1) CL2020002139A1 (en)
CO (1) CO2020010306A2 (en)
IL (1) IL276817A (en)
MA (1) MA52412A (en)
MX (1) MX2020008746A (en)
PE (1) PE20211456A1 (en)
PH (1) PH12020551343A1 (en)
RU (1) RU2020131012A (en)
SG (1) SG11202008291XA (en)
TW (1) TW202003518A (en)
WO (1) WO2019166432A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JOP20170169A1 (en) 2016-08-29 2019-01-30 Novartis Ag Fused tricyclic pyridazinone compounds useful to treat orthomyxovirus infections
KR102409595B1 (en) 2020-06-29 2022-06-17 한국과학기술연구원 Novel purinone derivatives as protein kinase CSF-1R inhibitor
CN112420196A (en) * 2020-11-20 2021-02-26 长沙市弘源心血管健康研究院 Prediction method and system for survival rate of acute myocardial infarction patient within 5 years
WO2024013205A1 (en) * 2022-07-14 2024-01-18 F. Hoffmann-La Roche Ag Phosphorylpurinone compounds for the treatment of cancer

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4189048B2 (en) 1997-12-26 2008-12-03 大日本住友製薬株式会社 Heterocyclic compounds
WO2010077613A1 (en) 2008-12-09 2010-07-08 Gilead Sciences, Inc. Modulators of toll-like receptors
EA201101650A1 (en) * 2009-05-21 2012-07-30 Астразенека Аб NEW PYRIMIDINE DERIVATIVES AND THEIR APPLICATION IN THE TREATMENT OF MALIGNANT NONFORMS AND THE FOLLOWING DISEASES
ES2644286T3 (en) * 2009-10-22 2017-11-28 Gilead Sciences, Inc. Purine or deazapurine derivatives useful for the treatment of (among others) viral infections
US20110150836A1 (en) * 2009-12-22 2011-06-23 Gilead Sciences, Inc. Methods of treating hbv and hcv infection
NZ604423A (en) * 2010-06-24 2015-01-30 Alkermes Pharma Ireland Ltd Prodrugs of nh-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
CA2807585A1 (en) * 2010-08-13 2012-02-16 Baylor Research Institute Novel vaccine adjuvants based on targeting adjuvants to antibodies directly to antigen-presenting cells
RU2745269C2 (en) * 2015-05-08 2021-03-22 Ф. Хоффманн-Ля Рош Аг New compounds and derivatives of sulfonimideoilpurinon for treatment and prophylaxis of viral infection
MA44334A (en) 2015-10-29 2018-09-05 Novartis Ag ANTIBODY CONJUGATES INCLUDING A TOLL-TYPE RECEPTOR AGONIST
MA46038B1 (en) * 2016-08-29 2021-05-31 Hoffmann La Roche Sulfonimidoylpurinone compounds substituted in the 7 position for the treatment and prophylaxis of viral infection
ES2894605T3 (en) * 2016-09-13 2022-02-15 Hoffmann La Roche Combination therapy with a TLR7 agonist and an HBV capsid assembly inhibitor

Also Published As

Publication number Publication date
CO2020010306A2 (en) 2020-08-31
JP2021514972A (en) 2021-06-17
WO2019166432A1 (en) 2019-09-06
IL276817A (en) 2020-10-29
CN111801100A (en) 2020-10-20
MX2020008746A (en) 2020-09-28
CN111801100B (en) 2023-10-24
AU2019228654A1 (en) 2020-09-03
MA52412A (en) 2021-06-02
CA3091950A1 (en) 2019-09-06
SG11202008291XA (en) 2020-09-29
BR112020016509A2 (en) 2020-12-15
RU2020131012A (en) 2022-03-28
PE20211456A1 (en) 2021-08-05
KR20200128414A (en) 2020-11-12
CL2020002139A1 (en) 2021-01-04
JP7089596B2 (en) 2022-06-22
TW202003518A (en) 2020-01-16
PH12020551343A1 (en) 2021-06-21
EP3758707A1 (en) 2021-01-06

Similar Documents

Publication Publication Date Title
AR114419A1 (en) 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PREVENTION OF LIVER CANCER
ECSP20067394A (en) CYCLINE-DEPENDENT KINASE INHIBITORS
DOP2018000187A (en) DERIVATIVES OF PIRAZOLO [1,5-A] PIRAZIN-4-ILO
CL2018000666A1 (en) New spiro compounds [3h-indole-3,2'-pyrrolidin] -2 (1h) -one and derivatives as inhibitors of mdm2-p53.
CO2021015698A2 (en) Modulators of thr-β and methods of using these
PE20190811A1 (en) DERIVATIVES OF PYRAZOLOPYRIMIDINES AS A KINASE INHIBITOR
AR120338A1 (en) PYRIDAZINONES AS PARP7 INHIBITORS
DOP2018000065A (en) DERIVATIVES OF 8- [6- [3- (AMINO) PROPOXI] -3-PIRIDIL] 1-ISOPROPILIMIDAZO [4,5-C] QUINOLIN-2-ONA AS SELECTED MODULATORS OF THE MUTED TELANGIECTASIA ATAXIA KINASE (ATM) FOR THE CANCER TREATMENT
AR111295A1 (en) PIRROLOPIRROL COMPOSITIONS AS PIRUVATO QUINASA ACTIVATORS (PKR)
CL2021002104A1 (en) Compounds, compositions and methods.
CL2017002207A1 (en) Transformation growth factor beta inhibitors (tgf-beta)
CO2019000932A2 (en) New 7-substituted sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of viral infection.
EA201792214A1 (en) COMPOUNDS OF SUBSTITUTE QUINAZOLINE
PH12016501066A1 (en) ROR GAMMA (ROYy) MODULATORS
AR070828A1 (en) DERIVATIVES OF AZETIDINE AND CYCLLOBUTANE AS JAK INHIBITORS
AR091490A1 (en) IAP ANTAGONISTS
AR119010A1 (en) COMPOUNDS, COMPOSITIONS AND METHODS OF USE
EA201991894A1 (en) PIPERIDINE-SUBSTITUTED Mnk INHIBITORS AND RELATED WAYS
AR122351A1 (en) METHYLQUINAZOLINONE DERIVATIVES AS BRAF INHIBITORS
AR109776A1 (en) P2X₃ AND / OR P2X₂ / ₃ COMPOUNDS AND METHODS
AR118768A1 (en) PYRIMIDINE DERIVATIVES AS INHIBITORS OF JAK KINASES
CO2024001285A2 (en) Tricyclic compounds as kras inhibitors
CL2019001023A1 (en) Naphthyridinone derivatives and their use in the treatment of arrhythmia.
CO2022004391A2 (en) 5-oxa-2–azaspiro[3.4]octane derivatives as m4 agonists
AR121878A1 (en) BENZODIAZEPINE DERIVATIVES AS GABAA PAM g1

Legal Events

Date Code Title Description
FB Suspension of granting procedure