HRP20131021T1 - Novi 7-deazapurin nukleozidi za terapijske uporabe - Google Patents
Novi 7-deazapurin nukleozidi za terapijske uporabe Download PDFInfo
- Publication number
- HRP20131021T1 HRP20131021T1 HRP20131021AT HRP20131021T HRP20131021T1 HR P20131021 T1 HRP20131021 T1 HR P20131021T1 HR P20131021A T HRP20131021A T HR P20131021AT HR P20131021 T HRP20131021 T HR P20131021T HR P20131021 T1 HRP20131021 T1 HR P20131021T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound according
- pharmaceutically acceptable
- hydrogen
- mixture
- acceptable salt
- Prior art date
Links
- 239000002777 nucleoside Substances 0.000 title claims 2
- 125000003835 nucleoside group Chemical group 0.000 title 1
- 230000001225 therapeutic effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 230000003287 optical effect Effects 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 229910052736 halogen Chemical group 0.000 claims 4
- 150000002367 halogens Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000012627 chemopreventive agent Substances 0.000 claims 2
- 229940124443 chemopreventive agent Drugs 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 239000012625 DNA intercalator Substances 0.000 claims 1
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims 1
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims 1
- 101000904173 Homo sapiens Progonadoliberin-1 Proteins 0.000 claims 1
- 102100024028 Progonadoliberin-1 Human genes 0.000 claims 1
- 101000996723 Sus scrofa Gonadotropin-releasing hormone receptor Proteins 0.000 claims 1
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims 1
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 229930013930 alkaloid Natural products 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 239000002870 angiogenesis inducing agent Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 230000002280 anti-androgenic effect Effects 0.000 claims 1
- 230000001772 anti-angiogenic effect Effects 0.000 claims 1
- 239000000051 antiandrogen Substances 0.000 claims 1
- 229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 claims 1
- 239000003080 antimitotic agent Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940034982 antineoplastic agent Drugs 0.000 claims 1
- 239000003886 aromatase inhibitor Substances 0.000 claims 1
- 229940046844 aromatase inhibitors Drugs 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 230000022131 cell cycle Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 235000011178 triphosphate Nutrition 0.000 claims 1
- 239000001226 triphosphate Substances 0.000 claims 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/14—Pyrrolo-pyrimidine radicals
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
Claims (13)
1. Spoj formule I:
[image]
gdje:
R1 je vodik, mono-, di-, ili tri-fosfat;
R2 je aril koji je po izboru supstituiran s jednim ili dva supstituenta izabrana iz grupe koja obuhvaća alkoksi, alkiltio, ili halogen;
R3 je vodik ili alkil; ili
njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili smjesa optičkih izomera.
2. Spoj prema zahtjevu 1, gdje R2 je aril koji je po izboru supstituiran jednim supstituentom izabranim iz grupe koja obuhvaća alkoksi, alkiltio, ili halogen; R3 je vodik; ili njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili smjesa optičkih izomera.
3. Spoj prema zahtjevu 1, gdje R1 je vodik, R2 je fenil koji je po izboru supstituiran jednim supstituentom izabranim iz grupe koja obuhvaća (C1-C4) alkoksi, (C1-C4) alkiltio, ili halogen; R3 je vodik; ili njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili smjesa optičkih izomera.
4. Spoj prema zahtjevu 1, gdje R3 je alkil; ili njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili smjesa optičkih izomera.
5. Spoj prema zahtjevu 1, gdje R1 je vodik, R2 je fenil koji je po izboru supstituiran jednim supstituentom izabranim iz grupe koja obuhvaća (C1-C4) alkoksi, (C1-C4) alkiltio, ili halogen; R3 je (C1-C4) alkil; ili njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili smjesa optičkih izomera.
6. Spoj prema zahtjevu 1 koji se izabire između sljedećih spojeva:
[image]
[image]
ili njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili smjesa optičkih izomera.
7. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku inhibicije rasta tumora/raka u subjekta.
8. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku inhibicije stanične proliferacije u stanicama tumora/raka u subjekta.
9. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku liječenja bolesti stanične proliferacije u subjekta.
10. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku liječenja neoplastične bolesti u subjekta.
11. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u postupku liječenja tumora ili raka u subjekta.
12. Farmaceutski pripravak koji sadrži terapijski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1 do 6 i jedan ili više farmaceutski prihvatljivih nosača.
13. Farmaceutski pripravak koji sadrži terapijski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1 do 6, i drugo terapijsko sredstvo izabrano iz grupe koja obuhvaća antracikline, DNA interkalatore, alkilirajuća sredstva, hormone, LHRH agoniste i antagoniste, inhibitore aromataze, antiandrogene, kemopreventivna sredstva, kemopreventivna sredstva staničnog ciklusa, antineoplastike, sredstva protiv mitoze, biljne alkaloide, inhibitore topoizomeraze I, inhibitore topoizomeraze II, inhibitore proteosoma, analoge nukleozida, citokine, faktore rasta, anti-angiogenične faktore, i jedan ili više farmaceutski prihvatljivih nosača.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17165609P | 2009-04-22 | 2009-04-22 | |
| PCT/CZ2010/000050 WO2010121576A2 (en) | 2009-04-22 | 2010-04-19 | Novel 7-deazapurine nucleosides for therapeutic uses |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20131021T1 true HRP20131021T1 (hr) | 2014-01-31 |
Family
ID=42768153
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20131021AT HRP20131021T1 (hr) | 2009-04-22 | 2013-10-28 | Novi 7-deazapurin nukleozidi za terapijske uporabe |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US9321800B2 (hr) |
| EP (1) | EP2421879B1 (hr) |
| JP (2) | JP5721275B2 (hr) |
| CN (2) | CN104497084B (hr) |
| AU (3) | AU2010238985B2 (hr) |
| CA (2) | CA2966647A1 (hr) |
| DK (1) | DK2421879T3 (hr) |
| ES (1) | ES2437917T3 (hr) |
| HK (2) | HK1166325A1 (hr) |
| HR (1) | HRP20131021T1 (hr) |
| MX (1) | MX2011011160A (hr) |
| NZ (2) | NZ700583A (hr) |
| PL (1) | PL2421879T3 (hr) |
| PT (1) | PT2421879E (hr) |
| SI (1) | SI2421879T1 (hr) |
| WO (1) | WO2010121576A2 (hr) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104497084B (zh) * | 2009-04-22 | 2018-06-05 | 捷克有机化学和生物化学研究院 | 用于治疗用途的7-脱氮嘌呤核苷 |
| CA2784596A1 (en) * | 2009-12-18 | 2011-06-23 | Joslin Diabetes Center, Inc. | Beta-cell replication promoting compounds and methods of their use |
| CN102319254B (zh) * | 2011-07-20 | 2013-06-19 | 上海交通大学 | 5-碘代杀菌核素在制备抗肿瘤药物中的应用 |
| CZ305466B6 (cs) * | 2013-11-04 | 2015-10-14 | Ústav organické chemie a biochemie Akademie věd České republiky, v. v. i. | Substituované 7-deazapurinové ribonukleosidy pro terapeutické použití |
| PL3218378T3 (pl) | 2014-11-14 | 2020-10-19 | Nerviano Medical Sciences S.R.L. | Pochodne 6-amino-7-bicyklo-7-deazapuryny jako inhibitory kinaz białkowych |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| WO2017197036A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| US10414788B2 (en) | 2016-06-29 | 2019-09-17 | Ustav Organicke Chemie A Biochemie Av Cr, V.V.I. | Substituted thienopyrrolopyrimidine ribonucleosides for therapeutic use |
| CZ307334B6 (cs) | 2016-08-02 | 2018-06-13 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | Substituované heteropentadieno-pyrrolopyrimidinové ribonukleosidy pro terapeutické použití |
| ES2948194T3 (es) | 2017-01-18 | 2023-09-01 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET |
| EP3697800A1 (en) | 2017-10-19 | 2020-08-26 | Universiteit Gent | Nucleoside analogues for the treatment of parasitic infections |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CN111971286B (zh) * | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| CN111630054B (zh) * | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| CZ308104B6 (cs) | 2018-03-12 | 2020-01-08 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v. v. i. | Pyridinopyrrolopyrimidinové ribonukleosidy pro terapeutické použití |
| WO2020033288A1 (en) * | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US11964988B2 (en) | 2018-09-10 | 2024-04-23 | Array Biopharma Inc. | Fused heterocyclic compounds as RET kinase inhibitors |
| MA56546A (fr) * | 2019-06-18 | 2022-04-27 | Taiho Pharmaceutical Co Ltd | Nouveau compose carbonate possedant un squelette pyrolo-pyrimidine ou sel pharmaceutiquement acceptable de celui-ci |
| WO2021164848A1 (en) * | 2020-02-17 | 2021-08-26 | Katholieke Universiteit Leuven | Novel 6-substituted 7-deazapurines and corresponding nucleosides as medicaments |
| EP4300796A1 (en) | 2021-02-26 | 2024-01-03 | Hitachi Industrial Products, Ltd. | Dynamo-electric machine |
| WO2023052468A1 (en) | 2021-09-28 | 2023-04-06 | Universiteit Antwerpen | Nucleoside analogues for the treatment of parasitic infections |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL108523A0 (en) * | 1993-02-03 | 1994-05-30 | Gensia Inc | Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain |
| EP2399588B1 (en) * | 2001-01-22 | 2020-04-29 | Merck Sharp & Dohme Corp. | Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase |
| WO2003051899A1 (en) * | 2001-12-17 | 2003-06-26 | Ribapharm Inc. | Deazapurine nucleoside libraries and compounds |
| AU2003232071A1 (en) * | 2002-05-06 | 2003-11-17 | Genelabs Technologies, Inc. | Nucleoside derivatives for treating hepatitis c virus infection |
| US20040157892A1 (en) | 2003-02-12 | 2004-08-12 | Crompton Co./Cie | Pesticidal fluoroethyl pyrazoles |
| US7169918B2 (en) * | 2003-10-27 | 2007-01-30 | Genelabs Technologies, Inc. | Methods for preparing 7-(2′-substituted-β-D-ribofuranosyl)-4-(NR2R3)-5-(substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine derivatives |
| JP2007509939A (ja) * | 2003-10-27 | 2007-04-19 | ジェネラブズ テクノロジーズ インコーポレーティッド | ウイルス感染を治療するためのヌクレオシド化合物 |
| US7202223B2 (en) * | 2003-10-27 | 2007-04-10 | Genelabs Technologies, Inc. | Nucleoside compounds for treating viral infections |
| EP1781101A2 (en) * | 2004-07-29 | 2007-05-09 | Metabasis Therapeutics, Inc. | Novel nucleoside derivatives |
| EP2231689B1 (en) * | 2008-01-18 | 2016-07-20 | Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic | Novel cytostatic 7-deazapurine nucleosides |
| ES2414159T3 (es) * | 2008-06-23 | 2013-07-18 | Janssen Pharmaceutica, N.V. | Antagonistas de acrilamida piperidilo de CCR2 |
| GB0815968D0 (en) * | 2008-09-03 | 2008-10-08 | Angeletti P Ist Richerche Bio | Antiviral agents |
| CN104497084B (zh) * | 2009-04-22 | 2018-06-05 | 捷克有机化学和生物化学研究院 | 用于治疗用途的7-脱氮嘌呤核苷 |
-
2010
- 2010-04-19 CN CN201410643709.3A patent/CN104497084B/zh active Active
- 2010-04-19 JP JP2012506333A patent/JP5721275B2/ja active Active
- 2010-04-19 WO PCT/CZ2010/000050 patent/WO2010121576A2/en active Application Filing
- 2010-04-19 PT PT107344335T patent/PT2421879E/pt unknown
- 2010-04-19 CA CA2966647A patent/CA2966647A1/en not_active Abandoned
- 2010-04-19 ES ES10734433.5T patent/ES2437917T3/es active Active
- 2010-04-19 DK DK10734433.5T patent/DK2421879T3/da active
- 2010-04-19 CN CN201080027802.1A patent/CN102459300B/zh active Active
- 2010-04-19 EP EP10734433.5A patent/EP2421879B1/en active Active
- 2010-04-19 AU AU2010238985A patent/AU2010238985B2/en active Active
- 2010-04-19 NZ NZ700583A patent/NZ700583A/en active IP Right Revival
- 2010-04-19 SI SI201030450T patent/SI2421879T1/sl unknown
- 2010-04-19 US US14/394,262 patent/US9321800B2/en active Active
- 2010-04-19 MX MX2011011160A patent/MX2011011160A/es active IP Right Grant
- 2010-04-19 PL PL10734433T patent/PL2421879T3/pl unknown
- 2010-04-19 NZ NZ596301A patent/NZ596301A/en unknown
- 2010-04-19 CA CA2759131A patent/CA2759131C/en active Active
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2012
- 2012-07-18 HK HK12107027.8A patent/HK1166325A1/xx unknown
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2013
- 2013-10-28 HR HRP20131021AT patent/HRP20131021T1/hr unknown
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2014
- 2014-10-20 JP JP2014213410A patent/JP6087889B2/ja active Active
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2015
- 2015-07-22 AU AU2015205885A patent/AU2015205885B2/en active Active
- 2015-10-08 HK HK15109842.4A patent/HK1209129A1/xx unknown
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2016
- 2016-03-17 US US15/073,502 patent/US9624257B2/en active Active
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2017
- 2017-03-08 US US15/453,702 patent/US10294262B2/en active Active
- 2017-06-19 AU AU2017204148A patent/AU2017204148B2/en active Active
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