HRP20120914T1 - Spojevi tetrahidrofuro[3,4-d]dioksolana, namijenjeni upotrebi u lijeäśenju virusnih infekcija i raka - Google Patents
Spojevi tetrahidrofuro[3,4-d]dioksolana, namijenjeni upotrebi u lijeäśenju virusnih infekcija i raka Download PDFInfo
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- HRP20120914T1 HRP20120914T1 HRP20120914AT HRP20120914T HRP20120914T1 HR P20120914 T1 HRP20120914 T1 HR P20120914T1 HR P20120914A T HRP20120914A T HR P20120914AT HR P20120914 T HRP20120914 T HR P20120914T HR P20120914 T1 HRP20120914 T1 HR P20120914T1
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- 208000036142 Viral infection Diseases 0.000 title claims 4
- 230000009385 viral infection Effects 0.000 title claims 4
- 206010028980 Neoplasm Diseases 0.000 title claims 2
- 201000011510 cancer Diseases 0.000 title claims 2
- 150000004862 dioxolanes Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 28
- -1 1,3-oxazol-2-yl Chemical group 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 6
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 5
- 108020004021 3-ketosteroid receptors Proteins 0.000 claims 5
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 claims 5
- 125000002252 acyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 108020000002 NR3 subfamily Proteins 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 2
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 2
- 125000005170 cycloalkyloxycarbonyl group Chemical group 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 2
- 125000005226 heteroaryloxycarbonyl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000005505 thiomorpholino group Chemical group 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims 1
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- MZAGXDHQGXUDDX-JSRXJHBZSA-N (e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/C(N)=O MZAGXDHQGXUDDX-JSRXJHBZSA-N 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- AAJXJLYUWKMQNO-UHFFFAOYSA-N 4-chloro-2-(1,2-oxazol-5-yl)phenol Chemical compound OC1=CC=C(Cl)C=C1C1=CC=NO1 AAJXJLYUWKMQNO-UHFFFAOYSA-N 0.000 claims 1
- 101100294106 Caenorhabditis elegans nhr-3 gene Proteins 0.000 claims 1
- 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 claims 1
- 201000011001 Ebola Hemorrhagic Fever Diseases 0.000 claims 1
- 241001115402 Ebolavirus Species 0.000 claims 1
- 241001466953 Echovirus Species 0.000 claims 1
- 241000709661 Enterovirus Species 0.000 claims 1
- 241000988559 Enterovirus A Species 0.000 claims 1
- 241000991587 Enterovirus C Species 0.000 claims 1
- 229940124683 HCV polymerase inhibitor Drugs 0.000 claims 1
- 241000711549 Hepacivirus C Species 0.000 claims 1
- 241000700721 Hepatitis B virus Species 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 1
- 241000700647 Variola virus Species 0.000 claims 1
- 241000710886 West Nile virus Species 0.000 claims 1
- 125000005090 alkenylcarbonyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- QWPPOHNGKGFGJK-UHFFFAOYSA-N hypochlorous acid Chemical group ClO QWPPOHNGKGFGJK-UHFFFAOYSA-N 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
Claims (24)
1. Spoj formule I:
[image]
,
naznačen time što:
B se bira između:
[image]
;
W je O, S ili NH;
X je N, Y je N, a Z je CH; ili X je N, Y je CR23, a Z je CH; ili X je C, Y je CR23, a Z je O;
R je OR3, SR3, NR3R4, NR3NR4R5, alkil, supstituirani alkil, alkenil, supstituirani alkenil, alkinil, supstituirani alkinil, aril, supstituirani aril, (CH2)n-CH(NHR3)CO2R4, (CH2)n-S-alkil, (CH2)n-S-aril, Cl, F, Br, I, CN, COOR3, CONR3R4, NHC(=NR3)NHR4, NR3OR4 NR3NO, NHCONHR3, NR3N=NR4, NR3N=CHR4, NR3C(O)NR4R5, NR3C(S)NR4R5, NR3C(O)OR4, CH=N-OR3, NR3C(=NH)NR4R5, NR3C(O)NR4NR5R6, O-C(O)R3, OC(O)-OR3, ONH-C(O)O-alkil, ONHC(O)O-aril, ONR3R4, SNR3R4, S-ONR3R4 ili SO2NR3R4; a R23 je H, CN, NO2, alkil, supstituirani alkil, alkenil, supstituirani alkenil, alkinil, supstituirani alkinil, CH=CF2, CH(=NR3)OR4, CHO, CH=CH-OCH3, NHCONH2, NHCSNH2, CONR3R4, CSNR3R4, CO2R3, alkoksi, NH2, alkilamino, dialkilamino, halogen, (1,3-oksazol-2-il), (1,3-oksazol-5-il), (1,3-tiazol-2-il), (imidazol-2-il), (2-okso[1,3]ditiol-4-il), (furan-2-il), (2H[1,2,3]triazol-4-il), C(=NH)NH2, C(=NH)NHOH, C(=NOH)NH2, acil, supstituirani acil, OR3, C(=NR3)R4, CH=NNR3R4, CH=NOR3, CH(OR3)2, B(OR3)2, C≡C-C(=O)NR3R4 ili N(=NHNH2)NHNH2; ili R i R23, zajedno s atomi na koje su vezani, mogu tvoriti cikloalkil, supstituirani cikloalkil, aril, supstituirani aril, heterocikloalkil, supstituirani heterocikloalkil, heteroaril ili supstituirani heteroaril;
n je 0-5;
R1 je H, NR3R4, Cl, F, OR3, SR3, NHCOR3, NHSO2R3, NHCONHR3, CN, alkil, aril, ONR3R4 ili NR3C(O)OR4;
R3, R4, R5 i R6 su neovisno bira iz skupine koju čine H, alkil, supstituirani alkil, alkenil, supstituirani alkenil, alkinil, supstituirani alkinil, cikloalkil, heterocikl, aril, supstituirani aril, acil, supstituirani acil, SO2-alkil i NO; ili R3 i R4, zajedno s dušikom na kojeg su vezani, tvore pirolidino, piperidino, piperazino, azetidino, morfolino ili tiomorfolino prsten; ili R4 i R5, zajedno s dušikom na kojeg su vezani, tvore pirolidino, piperidino, piperazino, azetidino, morfolino ili tiomorfolino prsten;
Ra se bira iz skupine koju čine vodik, C1-6 alkilkarbonil, C2-18 alkenilkarbonil, C1-10 alkiloksikarbonil, C3-6 cikloalkilkarbonil, C3-6 cikloalkiloksikarbonil, arilkarbonil, ariloksikarbonil, heteroarilkarbonil, heteroariloksikarbonil, aminoacilni ostatak strukturne formule -C(=O)CH(R11)NH-R12, ili ostatak strukturne formule: -P(=O)(OAr)-NHCH(R13)-C(=O)OR14, gdje su alkilkarbonil, alkiloksikarbonil, cikloalkilkarbonil i cikloalkiloksikarbonil nesupstituirani ili su supstituirani s jednim do tri supstituenta, koje se neovisno bira iz skupine koju čine halogen, hidroksi, karboksi, C1-4 alkoksi, amino, C1-4 alkilamino i di(C1-4 alkil)amino, te gdje su arilkarbonil, ariloksikarbonil, heteroarilkarbonil i heteroariloksikarbonil nesupstituirani ili su supstituirani s jednim do pet supstituenata, koje se neovisno bira između R9;
Ar je fenil, koji je nesupstituiran ili je supstituiran s jednim do tri supstituenta, koje se neovisno bira iz skupine koju čine halogen, C1-4 alkil, C1-4 alkoksi, C1-4 alkiltio, cijano, nitro, amino, karboksi, trifluormetil, C1-4 alkilamino, di(C1-4 alkil)amino, C1-4 alkilkarbonil, C1-4 alkilkarboniloksi i C1-4 alkiloksikarbonil;
svaki R9 se neovisno bira iz skupine koju čine halogen, C1-4 alkil, C1-4 alkoksi, C1-4 alkiltio, C1-4 alkilsulfonil, cijano, nitro, amino, fenil, karboksi, trifluormetil, difluormetoksi, trifluormetoksi, C1-4 alkilamino, di(C1-4 alkil)amino, C1-4 alkilkarbonil, C1-4 alkilkarboniloksi i C1-4 alkiloksikarbonil;
R11 je vodik, C1-5 alkil ili fenil C0-2 alkil;
R12 je vodik, C1-4 alkil, C1-4 acil, benzoil, C1-4 alkiloksikarbonil, fenil C0-2 alkiloksikarbonil, C1-4 alkilaminokarbonil, fenil C0-2 alkilaminokarbonil, C1-4 alkilsulfonil ili fenil C0-2 alkilsulfonil;
R13 je vodik, C1-5 alkil, fenil ili benzil; gdje je alkil nesupstituiran ili je supstituiran s jednim supstituentom, kojeg se bira iz skupine koju čine hidroksi, metoksi, amino, karboksi, karbamoil, guanidino, merkapto, metiltio, 1H-imidazolil i 1H-indol-3-il; te gdje su fenil i benzil nesupstituirani ili su supstituirani s jednim do dva supstituenta, koje se neovisno bira iz skupine koju čine halogen, hidroksi i metoksi;
R14 je vodik, C1-6 alkil, C3-6 cikloalkil, fenil ili benzil; gdje su alkil i cikloalkil nesupstituirani ili su supstituirani s jednim do tri supstituenta, koje se neovisno bira između halogena, hidroksi, karboksi, C1-4 alkoksi; te gdje su fenil i benzil nesupstituirani ili su supstituirani s jednim do tri supstituenta, koje se neovisno bira između halogena, hidroksi, cijano, C1-4 alkoksi i trifluormetila;
Rb se bira iz skupine koju čine C1-12 alkil, C3-8 cikloalkil, aril, i heteroaril; gdje su alkil i cikloalkil nesupstituirani ili su supstituirani s jednim do tri supstituenta, koje se neovisno bira između halogena, hidroksi, karboksi i C1-4 alkoksi; a aril i heteroaril su nesupstituirani ili su supstituirani s jednim do pet supstituenata, koje se neovisno bira između R9; i
Rc se bira iz skupine koju čine vodik, alkil, alkenil i alkenil, gdje je svaki alkil, alkenil i alkinil izborno supstituiran s jednim ili više supstituenata, koje se neovisno bira između halo, amino, hidroksi i alkoksi;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što W je O.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što W je S.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što R je OR3, Cl, SR3, NR3R4 ili NR3NR4R5.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što R je hidroksi, klor, metoksi, merkapto, amino, metilamino, izopropilamino, propilamino, etilamino, dimetilamino, ciklopropilamino, 2-aminoetilamino, 1-(2-hidroksietil)hidrazino, hidrazino, 1-metilhidrazino, azetidino ili pirolidino.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što R1 je H ili NR3R4.
7. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule Ia:
[image]
,
gdje se Rb bira između:
[image]
[image]
[image]
-CH2CH3, -(CH2)5CH3,
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule Ib:
[image]
,
gdje se Rb bira između:
[image]
[image]
[image]
-CH2CH3, -(CH2)5CH3,
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (Ic):
[image]
,
gdje se Ra bira između
[image]
[image]
[image]
[image]
i
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (Id):
[image]
,
gdje se Ra bira između
[image]
[image]
[image]
[image]
i
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (Ie):
[image]
,
gdje se Rb bira između:
[image]
[image]
[image]
-CH2CH3, -(CH2)5CH3,
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (If):
[image]
,
gdje se Rb bira između:
[image]
[image]
[image]
-CH2CH3, -(CH2)5CH3,
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (Ig):
[image]
,
gdje se Ra bira između
[image]
[image]
[image]
[image]
i
[image]
ili njegova farmaceutski prihvatljiva sol.
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (Ih):
[image]
,
gdje se Ra bira između
[image]
[image]
[image]
[image]
i
[image]
ili njegova farmaceutski prihvatljiva sol.
15. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-14, kao i farmaceutski prihvatljivu podlogu.
16. Pripravak u skladu s patentnim zahtjevom 15, naznačen time što dodatno sadrži jedno ili više dodatnih antivirusnih sredstava.
17. Pripravak u skladu s patentnim zahtjevom 15 ili 16, naznačen time što dodatno sadrži jedan ili više dodatnih inhibitora HCV polimeraze.
18. Pripravak u skladu s bilo kojim od patentnih zahtjeva 15-17, naznačen time što dodatno sadrži jedan ili više inhibitora proteaze.
19. Pripravak u skladu s bilo kojim od patentnih zahtjeva 15-18, naznačen time što dodatno sadrži jedno ili više sredstava protiv raka.
20. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-14, naznačen time što je namijenjen upotrebi u terapiji.
21. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-14, naznačen time što je namijenjen upotrebi u liječenju virusne infekcije kod životinje.
22. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-14, naznačen time što je namijenjen upotrebi u liječenju raka kod životinje.
23. Spoj u skladu s patentnim zahtjevom 21, naznačen time što se virusnu infekciju bira iz skupine koju čine: virus hepatitisa B, virus hepatitisa C, virus ljudske imunodeficijencije, poliovirus, coxsackie virus A i B, rinovirus, ECHO-virus, velike boginje, Ebola i virus zapadnog Nila.
24. Spoj u skladu s patentnim zahtjevom 21, naznačen time što je virusna infekcija HCV.
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| US91721007P | 2007-05-10 | 2007-05-10 | |
| US94012507P | 2007-05-25 | 2007-05-25 | |
| PCT/US2008/063037 WO2008141079A1 (en) | 2007-05-10 | 2008-05-08 | Tetrahydrofuro [3 4-d] dioxolane compounds for use in the treatment of viral infections and cancer |
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| HRP20120914AT HRP20120914T1 (hr) | 2007-05-10 | 2012-11-13 | Spojevi tetrahidrofuro[3,4-d]dioksolana, namijenjeni upotrebi u lijeäśenju virusnih infekcija i raka |
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| US (1) | US8242085B2 (hr) |
| EP (1) | EP2155758B1 (hr) |
| JP (1) | JP2011513195A (hr) |
| AU (1) | AU2008251555B2 (hr) |
| CA (1) | CA2685520A1 (hr) |
| CY (1) | CY1113323T1 (hr) |
| DK (1) | DK2155758T3 (hr) |
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| HK (1) | HK1139656A1 (hr) |
| HR (1) | HRP20120914T1 (hr) |
| PL (1) | PL2155758T3 (hr) |
| PT (1) | PT2155758E (hr) |
| WO (1) | WO2008141079A1 (hr) |
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| TW200942243A (en) | 2008-03-05 | 2009-10-16 | Biocryst Pharm Inc | Antiviral therapeutic agents |
| US20090247750A1 (en) * | 2008-03-28 | 2009-10-01 | Biocryst Pharmaceuticals, Inc. | Process for preparing nucleoside analogs |
| PT2268642E (pt) * | 2008-04-23 | 2015-06-02 | Gilead Sciences Inc | Análogos de carba-nulceósidos 1¿-substituídos para tratamento antiviral |
| WO2010036407A2 (en) * | 2008-05-15 | 2010-04-01 | Biocryst Pharmaceuticals, Inc. | Antiviral nucleoside analogs |
| EP2313102A2 (en) | 2008-07-03 | 2011-04-27 | Biota Scientific Management | Bycyclic nucleosides and nucleotides as therapeutic agents |
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| WO2011035250A1 (en) | 2009-09-21 | 2011-03-24 | Gilead Sciences, Inc. | Processes and intermediates for the preparation of 1'-substituted carba-nucleoside analogs |
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2008
- 2008-05-08 PL PL08747850T patent/PL2155758T3/pl unknown
- 2008-05-08 ES ES08747850T patent/ES2393038T3/es active Active
- 2008-05-08 AU AU2008251555A patent/AU2008251555B2/en not_active Ceased
- 2008-05-08 EP EP08747850A patent/EP2155758B1/en not_active Not-in-force
- 2008-05-08 WO PCT/US2008/063037 patent/WO2008141079A1/en active Application Filing
- 2008-05-08 CA CA002685520A patent/CA2685520A1/en not_active Abandoned
- 2008-05-08 US US12/599,656 patent/US8242085B2/en active Active
- 2008-05-08 PT PT08747850T patent/PT2155758E/pt unknown
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- 2008-05-08 JP JP2010507652A patent/JP2011513195A/ja active Pending
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2010
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2012
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- 2012-11-13 HR HRP20120914AT patent/HRP20120914T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DK2155758T3 (da) | 2012-11-05 |
| HK1139656A1 (en) | 2010-09-24 |
| PL2155758T3 (pl) | 2013-06-28 |
| WO2008141079A1 (en) | 2008-11-20 |
| AU2008251555B2 (en) | 2012-08-30 |
| CA2685520A1 (en) | 2008-11-20 |
| PT2155758E (pt) | 2012-11-12 |
| US20110002886A1 (en) | 2011-01-06 |
| AU2008251555A1 (en) | 2008-11-20 |
| EP2155758B1 (en) | 2012-08-22 |
| JP2011513195A (ja) | 2011-04-28 |
| US8242085B2 (en) | 2012-08-14 |
| CY1113323T1 (el) | 2016-06-22 |
| EP2155758A1 (en) | 2010-02-24 |
| ES2393038T3 (es) | 2012-12-18 |
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