PE20211456A1 - 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND ITS DERIVATIVES FOR THE TREATMENT AND PREVENTION OF LIVER CANCER - Google Patents
7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND ITS DERIVATIVES FOR THE TREATMENT AND PREVENTION OF LIVER CANCERInfo
- Publication number
- PE20211456A1 PE20211456A1 PE2020001228A PE2020001228A PE20211456A1 PE 20211456 A1 PE20211456 A1 PE 20211456A1 PE 2020001228 A PE2020001228 A PE 2020001228A PE 2020001228 A PE2020001228 A PE 2020001228A PE 20211456 A1 PE20211456 A1 PE 20211456A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- prevention
- derivatives
- treatment
- substituted
- Prior art date
Links
Classifications
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- 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
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- 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
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- 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
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- 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 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
Referido a un compuesto de formula I, en donde R1 es alquilo-C1-6; R2 es bencilo, en donde no esta sustituido o esta sustituido con uno, dos o tres sustituyentes seleccionados independientemente de halogeno 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, entre otros; o una sal farmaceuticamente aceptable, enantiomero o diastereomero del mismo. Un compuesto seleccionado es 6-amino-9-bencil-N-metil-8-oxo-N-propil-2-(propilsulfonimidoil)purin-7-carboxamida. Estos compuestos de sulfonimidoilpurinona 7-sustituidos y sus derivados tienen actividad agonista del receptor tipo Toll (TLR) in vivo, son utilizados en el tratamiento y prevencion del cancer de higado. Tambien se refiere a compuestos intermedios, preparacion de los mismos, composicion farmaceutica que comprende dicho compuesto en combinacion con un anticuerpo antagonista de PD1 o un anticuerpo antagonista de PD-L1.Referred to a compound of formula I, wherein R1 is C1-6 alkyl; R2 is benzyl, where it is unsubstituted or substituted with one, two, or three substituents independently selected from halogen and C1-6alkyl; R3 is -NR4R5, wherein R4 is -C 1-6 alkyl or -C 1-6 alkoxy-C1-6 alkyl; R5 is (C1-6 alkyl) 2NCOO-C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, among others; or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof. A selected compound is 6-amino-9-benzyl-N-methyl-8-oxo-N-propyl-2- (propylsulfonimidoyl) purine-7-carboxamide. These 7-substituted sulfonimidoylpurinone compounds and their derivatives have Toll-like receptor (TLR) agonist activity in vivo, they are used in the treatment and prevention of liver cancer. It also refers to intermediates, preparation thereof, pharmaceutical composition comprising said compound in combination with a PD1 antagonist antibody or a PD-L1 antagonist antibody.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018077501 | 2018-02-28 | ||
| PCT/EP2019/054729 WO2019166432A1 (en) | 2018-02-28 | 2019-02-26 | 7-substituted sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of liver cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211456A1 true PE20211456A1 (en) | 2021-08-05 |
Family
ID=65685310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020001228A PE20211456A1 (en) | 2018-02-28 | 2019-02-26 | 7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND ITS 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)
| 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)
| 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 |
| ES2623794T3 (en) | 2008-12-09 | 2017-07-12 | Gilead Sciences, Inc. | Intermediates for the preparation of toll receptor modulators |
| WO2010133885A1 (en) * | 2009-05-21 | 2010-11-25 | Astrazeneca Ab | Novel pyrimidine derivatives and their use in the treatment of cancer and further diseases |
| NO2491035T3 (en) * | 2009-10-22 | 2018-01-27 | ||
| US20110150836A1 (en) * | 2009-12-22 | 2011-06-23 | Gilead Sciences, Inc. | Methods of treating hbv and hcv infection |
| AU2011270701B2 (en) * | 2010-06-24 | 2015-05-14 | Alkermes Pharma Ireland Limited | Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives |
| BR112013002940A2 (en) * | 2010-08-13 | 2019-09-24 | Baylor Res Institute | new vaccine adjuvants based on targeting adjuvants for antibodies directly to 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 |
| NZ750604A (en) * | 2016-08-29 | 2024-02-23 | Hoffmann La Roche | Novel 7-substituted sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of virus infection |
| ES2894605T3 (en) * | 2016-09-13 | 2022-02-15 | Hoffmann La Roche | Combination therapy with a TLR7 agonist and an HBV capsid assembly inhibitor |
-
2019
- 2019-02-26 SG SG11202008291XA patent/SG11202008291XA/en unknown
- 2019-02-26 JP JP2020544794A patent/JP7089596B2/en active Active
- 2019-02-26 RU RU2020131012A patent/RU2020131012A/en unknown
- 2019-02-26 BR BR112020016509-3A patent/BR112020016509A2/en not_active Application Discontinuation
- 2019-02-26 CA CA3091950A patent/CA3091950A1/en active Pending
- 2019-02-26 EP EP19708981.6A patent/EP3758707A1/en active Pending
- 2019-02-26 MX MX2020008746A patent/MX2020008746A/en unknown
- 2019-02-26 AU AU2019228654A patent/AU2019228654A1/en not_active Abandoned
- 2019-02-26 KR KR1020207027935A patent/KR20200128414A/en unknown
- 2019-02-26 MA MA052412A patent/MA52412A/en unknown
- 2019-02-26 WO PCT/EP2019/054729 patent/WO2019166432A1/en unknown
- 2019-02-26 CN CN201980015912.7A patent/CN111801100B/en active Active
- 2019-02-26 PE PE2020001228A patent/PE20211456A1/en unknown
- 2019-02-27 TW TW108106752A patent/TW202003518A/en unknown
- 2019-02-28 AR ARP190100505A patent/AR114419A1/en unknown
-
2020
- 2020-08-19 IL IL276817A patent/IL276817A/en unknown
- 2020-08-19 CL CL2020002139A patent/CL2020002139A1/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 |
|---|---|
| SG11202008291XA (en) | 2020-09-29 |
| EP3758707A1 (en) | 2021-01-06 |
| CN111801100B (en) | 2023-10-24 |
| BR112020016509A2 (en) | 2020-12-15 |
| CN111801100A (en) | 2020-10-20 |
| CA3091950A1 (en) | 2019-09-06 |
| CL2020002139A1 (en) | 2021-01-04 |
| AR114419A1 (en) | 2020-09-02 |
| JP7089596B2 (en) | 2022-06-22 |
| JP2021514972A (en) | 2021-06-17 |
| RU2020131012A (en) | 2022-03-28 |
| AU2019228654A1 (en) | 2020-09-03 |
| MX2020008746A (en) | 2020-09-28 |
| KR20200128414A (en) | 2020-11-12 |
| IL276817A (en) | 2020-10-29 |
| WO2019166432A1 (en) | 2019-09-06 |
| CO2020010306A2 (en) | 2020-08-31 |
| PH12020551343A1 (en) | 2021-06-21 |
| MA52412A (en) | 2021-06-02 |
| TW202003518A (en) | 2020-01-16 |
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