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 CANCERInfo
- 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
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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Genetics & Genomics (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (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.
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 (5)
| 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 |
| PE20210403A1 (en) | 2018-02-28 | 2021-03-02 | Novartis Ag | DERIVATIVES OF 10- (DI (PHENYL) METHYL) -4-HYDROXY-8,9,9A, 10-TETRAHYDRO-7H-PYRROLO [1 ', 2': 4,5] PIRAZINE [1,2-B] PYRIDAZINE- 3,5-DIONA AND RELATED COMPOUNDS AS INHIBITORS OF THE REPLICATION OF ORTHOMYXOVIRUS FOR THE TREATMENT OF INFLUENZA |
| 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)
| 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 |
| EA021377B9 (en) | 2008-12-09 | 2015-09-30 | Джилид Сайэнс, Инк. | Modulators of toll-like receptors |
| MX2011012337A (en) * | 2009-05-21 | 2011-12-08 | Dainippon Sumitomo Pharma Co | Novel pyrimidine derivatives and their use in the treatment of cancer and further diseases. |
| SI2491035T1 (en) * | 2009-10-22 | 2017-10-30 | Gilead Sciences, Inc. | Derivatives of purine or deazapurine useful for the treatment of (inter alia) 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 |
| AR082686A1 (en) * | 2010-08-13 | 2012-12-26 | Baylor Res Inst | VACCINE ASSISTANTS DIRECTING ANTIBODY ADJUSTERS DIRECTLY TOWARDS ANTIGEN PRESENTING CELLS |
| UA120450C2 (en) | 2015-05-08 | 2019-12-10 | Ф. Хоффманн-Ля Рош Аг | Novel sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of virus infection |
| MA44334A (en) | 2015-10-29 | 2018-09-05 | Novartis Ag | ANTIBODY CONJUGATES INCLUDING A TOLL-TYPE RECEPTOR AGONIST |
| SI3504210T1 (en) * | 2016-08-29 | 2021-08-31 | F. Hoffmann-La Roche Ag | 7-substituted sulfonimidoylpurinone compounds for the treatment and prophylaxis of virus infection |
| EP3970750A1 (en) * | 2016-09-13 | 2022-03-23 | F. Hoffmann-La Roche AG | Combined treatment with a tlr7 agonist and an hbv capsid assembly inhibitor |
-
2019
- 2019-02-26 RU RU2020131012A patent/RU2020131012A/en unknown
- 2019-02-26 EP EP19708981.6A patent/EP3758707A1/en active Pending
- 2019-02-26 AU AU2019228654A patent/AU2019228654A1/en not_active Abandoned
- 2019-02-26 PE PE2020001228A patent/PE20211456A1/en unknown
- 2019-02-26 MA MA052412A patent/MA52412A/en unknown
- 2019-02-26 JP JP2020544794A patent/JP7089596B2/en active Active
- 2019-02-26 CA CA3091950A patent/CA3091950A1/en active Pending
- 2019-02-26 MX MX2020008746A patent/MX2020008746A/en unknown
- 2019-02-26 BR BR112020016509-3A patent/BR112020016509A2/en not_active Application Discontinuation
- 2019-02-26 CN CN201980015912.7A patent/CN111801100B/en active Active
- 2019-02-26 KR KR1020207027935A patent/KR20200128414A/en not_active Application Discontinuation
- 2019-02-26 WO PCT/EP2019/054729 patent/WO2019166432A1/en active Application Filing
- 2019-02-26 SG SG11202008291XA patent/SG11202008291XA/en unknown
- 2019-02-27 TW TW108106752A patent/TW202003518A/en unknown
- 2019-02-28 AR ARP190100505A patent/AR114419A1/en unknown
-
2020
- 2020-08-19 CL CL2020002139A patent/CL2020002139A1/en unknown
- 2020-08-19 IL IL276817A patent/IL276817A/en unknown
- 2020-08-21 CO CONC2020/0010306A patent/CO2020010306A2/en unknown
- 2020-08-27 PH PH12020551343A patent/PH12020551343A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL276817A (en) | 2020-10-29 |
| WO2019166432A1 (en) | 2019-09-06 |
| BR112020016509A2 (en) | 2020-12-15 |
| JP7089596B2 (en) | 2022-06-22 |
| CL2020002139A1 (en) | 2021-01-04 |
| RU2020131012A (en) | 2022-03-28 |
| EP3758707A1 (en) | 2021-01-06 |
| TW202003518A (en) | 2020-01-16 |
| PH12020551343A1 (en) | 2021-06-21 |
| SG11202008291XA (en) | 2020-09-29 |
| MA52412A (en) | 2021-06-02 |
| AU2019228654A1 (en) | 2020-09-03 |
| CN111801100A (en) | 2020-10-20 |
| PE20211456A1 (en) | 2021-08-05 |
| JP2021514972A (en) | 2021-06-17 |
| CO2020010306A2 (en) | 2020-08-31 |
| CN111801100B (en) | 2023-10-24 |
| KR20200128414A (en) | 2020-11-12 |
| MX2020008746A (en) | 2020-09-28 |
| CA3091950A1 (en) | 2019-09-06 |
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