HRP20220710T1 - Antiproliferacijski spojevi i njihova uporaba - Google Patents
Antiproliferacijski spojevi i njihova uporaba Download PDFInfo
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- HRP20220710T1 HRP20220710T1 HRP20220710TT HRP20220710T HRP20220710T1 HR P20220710 T1 HRP20220710 T1 HR P20220710T1 HR P20220710T T HRP20220710T T HR P20220710TT HR P20220710 T HRP20220710 T HR P20220710T HR P20220710 T1 HRP20220710 T1 HR P20220710T1
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- 150000001875 compounds Chemical class 0.000 title claims 35
- 230000001028 anti-proliverative effect Effects 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 36
- 229910052757 nitrogen Inorganic materials 0.000 claims 30
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 27
- 125000005842 heteroatom Chemical group 0.000 claims 27
- 229910052760 oxygen Inorganic materials 0.000 claims 27
- 239000001301 oxygen Chemical group 0.000 claims 27
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 24
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 22
- 125000001931 aliphatic group Chemical group 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 20
- 239000011593 sulfur Chemical group 0.000 claims 20
- 229910052717 sulfur Chemical group 0.000 claims 20
- 229920006395 saturated elastomer Polymers 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 6
- 125000002950 monocyclic group Chemical group 0.000 claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 210000002472 endoplasmic reticulum Anatomy 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 230000001939 inductive effect Effects 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 239000005864 Sulphur Substances 0.000 claims 2
- 102100036022 Wolframin Human genes 0.000 claims 2
- 108050007567 Wolframin Proteins 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 230000004906 unfolded protein response Effects 0.000 claims 2
- 102000018441 wolframin Human genes 0.000 claims 2
- -1 -C(O)OC1-4aliphatic Chemical group 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
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- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (20)
1. Spoj formule I’:
[image]
ili njegova farmaceutski prihvatljiva sol, naznačeno time, da:
prsten A je prsten odabran između fenila, 5-7-eročlanog zasićenog ili djelomično nezasićenog karbocikličkog prstena, 8-12-eročlanog zasićenog ili djelomično nezasićenog bicikličkog heterocikličkog prstena koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora, 5- 6-eročlanog heteroaromatskog prstena koji ima 1-4 heteroatoma neovisno odabrana od dušika, kisika ili sumpora; ili 8-10-eročlanog bicikličkog heteroaromatskog prstena koji ima 1-5 heteroatoma neovisno odabrana od dušika, kisika ili sumpora;
svaki R1 je neovisno vodik, ili alifatski C1-3 po izboru supstituiran s 1-6 halogenom; ili
dvije R1 skupine su po izboru uzete zajedno s njihovim intervenirajućim atomima kako bi tvorile 5-8 eročlani djelomično nezasićeni kondenzirani karbociklički prsten;
svaki od R2 je neovisno vodik, halogen, -CN, -NO2, -C(O)OR, -C(O)NR2, -NR2, -NRC(O)R, -NRC(O)OR, -NRS(O)2R, -OR, -P(O)R2, -SR, -S(O)R, -S(O)2R, -S(O)(NH)R, -S(O)2NR2 ili R; ili
dvije R2 skupine su po izboru uzete zajedno kako bi tvorile =O; ili
dvije R2 skupine su po izboru uzete zajedno s njihovim intervenirajućim atomima kako bi tvorile 3-8-eročlani zasićeni spirociklički prsten koji ima 0-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora;
svaki R3 je neovisno vodik, -OH ili alifatski C1-3; ili
dvije R3 grupe su po izboru uzete zajedno kako bi tvorile =O; ili
dvije R3 grupe su po izboru uzete zajedno kako bi tvorile =CH2; ili
dvije R3 skupine su po izboru uzete zajedno s njihovim intervenirajućim atomima kako bi tvorile 3-8-eročlani zasićeni spirociklički prsten koji ima 0-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora; ili
dvije R3 skupine su po izboru uzete zajedno s njihovim intervenirajućim atomima kako bi tvorile 5-8-eročlani zasićeni premošteni biciklički prsten koji ima 0-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora;
svaki R je neovisno vodik ili po izboru supstituirana skupina odabrana između alifatskog C1-6, 3-8-eročlanog zasićenog ili djelomično nezasićenog monocikličkog karbocikličkog prstena, fenila, 7-10-eročlanog zasićenog spirobicikličkog heterocikličkog prstena koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora, 7-10-eročlanog zasićenog ili djelomično nezasićenog kondenziranog bicikličkog heterocikličkog prstena koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora, 4-8-eročlanog zasićenog ili djelomično nezasićenog monocikličkog heterocikličkog prstena koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora ili 5-6-eročlanog monocikličkog heteroaromatskog prstena koji ima 1-4 heteroatoma neovisno odabrana od dušika, kisika ili sumpora; ili:
dvije R skupine na istom dušiku su po izboru uzete zajedno sa svojim atomima koji su među njima kako bi tvorile 4-7-eročlani zasićeni, djelomično nezasićeni ili heteroarilni prsten koji ima 0-3 heteroatoma, osim dušika, neovisno odabrana od dušika, kisika i sumpora, po izboru supstituiran s 1-2 okso skupine;
------ je jednostruka ili dvostruka veza;
X je -O-, -N(R)-, -N(S(O)2(R))-, -S-, -S(O)-, -S(O)2-, -CH2-, -CH(R3)-, ili -C(R3)2-;
m je 0, 1 ili 2;
n je 0, 1, 2, 3, 4 ili 5; i
p je 0, 1 ili 2.
2. Spoj u skladu s patentnim zahtjevom 1 ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je prsten A fenil; ili:
pri čemu je prsten A 8-12-eročlani zasićeni ili djelomično nezasićeni biciklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora; ili:
pri čemu je prsten A 8-10-eročlani biciklički heteroaromatski prsten koji ima 1-5 heteroatoma neovisno odabrana od dušika, kisika ili sumpora; ili:
pri čemu je prsten A
[image]
pri čemu je prsten B 5-7-eročlani djelomično nezasićeni heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora, ili je prsten B 5-6-eročlani heteroaromatski prsten koji ima 1-4 heteroatoma neovisno odabrana od dušika, kisika ili sumpora; ili:
pri čemu se prsten A bira između:
[image]
[image]
[image]
i
[image]
3. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2 ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je najmanje jedan od R1 alifatski C1-3 ; ili:
gdje je najmanje jedan od R1 -CH3; i/ili:
pri čemu je najmanje jedan od R1 vezan na položaj 6 pirimidina.
4. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je najmanje jedan od R2 alifatski C1-6, po izboru supstituiran 1-4 puta halogenom, -OH, NH2, -OCH3, -NHC (O)CH3, -S(O)2CH3, -COOH, -CO2CH3, -CO2C2H5 ili -N(CH3)C(O)CH3; po izboru: pri čemu je najmanje jedan od R2 odabran od -CH3, -CF3, -CH2CH3, -C≡CH,
[image]
[image]
[image]
i
[image]
ili
pri čemu je najmanje jedan od R2 3-6-eročlani zasićeni monociklički karbociklički prsten; po izboru:
pri čemu je barem jedan od R2
[image]
ili: pri čemu je najmanje jedan od R2 7-10-eročlani zasićeni spirobiciklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika ili kisika; po izboru:
pri čemu je najmanje jedan od R2 odabran od
[image]
i
[image]
ili
pri čemu je najmanje jedan od R2 7-10-eročlani zasićeni kondenzirani biciklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika ili kisika; po izboru:
pri čemu je barem jedan od R2
[image]
ili: pri čemu je barem jedan od R2 4-6-eročlani zasićeni monociklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora, po izboru supstituiran 1-4 puta halogenom, -OH, -CH3, -OCH3 , =O,
[image]
[image]
ili
[image]
po izboru:
pri čemu je najmanje jedan od R2 odabran od
[image]
[image]
[image]
[image]
i
[image]
ili: gdje je najmanje jedan od R2 5-6-eročlani monociklički heteroaromatski prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora; po izboru:
pri čemu je najmanje jedan od R2 odabran od
[image]
i
[image]
ili:
pri čemu je najmanje jedan od R2 -C(O)OR, gdje je R vodik ili alifatski C1-6; po izboru:
pri čemu je najmanje jedan od R2 -C(O)OH,
[image]
ili
[image]
ili: pri čemu je najmanje jedan od R2 -C(O)NR2, pri čemu je svaki od R neovisno vodik, alifatski C1-6 koji je po izboru supstituiran s -N(CH3)2, nesupstituiranim 3-6-eročlanim zasićenim monocikličkim karbocikličkim prstenom ili nesupstituiranim 4-6-eročlani zasićenim monocikličkim heterocikličkim prstenom koji ima 1-2 heteroatoma neovisno odabrana od dušika ili kisika, ili dva R uzeti zajedno s njihovim intervenirajućim atomima kako bi tvorili 4-7-eročlani zasićeni i nesupstituirani prsten koji ima 0-3 heteroatoma, koji osim dušika, je neovisno odabran od dušika, kisika i sumpora; po izboru:
pri čemu je najmanje jedan od R2 odabran od
[image]
[image]
i
[image]
ili: pri čemu je najmanje jedan od R2 -NR2, gdje je svaki od R neovisno: vodik;
alifatski C1-6 koji je po izboru supstituiran 1-2 puta s -OH,
[image]
ili
[image]
nesupstituirani 3-6-eročlani zasićeni monociklički karbociklički prsten;
4-6-eročlani zasićeni monociklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika ili kisika, koji je po izboru 1-2 puta supstituiran s CH3, -OH, -C(O)OC(CH3)3 ili -C(C)CH3; ili 6-eročlani monociklički heteroaromatski prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora koji je po izboru supstituiran 1-2 puta sa -CH3 ili -NH2; po izboru:
pri čemu je najmanje jedan od R2 odabran od:
[image]
[image]
[image]
[image]
i
[image]
5. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačeno time, da najmanje jedan od R2 je -NHC(O)R, gdje je R alifatski C1-6, po izboru supstituiran 1-3 puta s halogenom, - OCH3, -N(CH3)2 ili -OH, 3-6-eročlani zasićeni monociklički karbociklički prsten po izboru supstituiran 1-2 puta s halogenom ili -OH, ili 4-6-eročlani zasićeni monociklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora po izboru supstituirana 1-2 puta s halogenom, -OH ili -CH3; po izboru:
kada je najmanje jedan od R2 odabran od
[image]
[image]
[image]
[image]
[image]
i
[image]
ili:
pri čemu je najmanje jedan od R2 -NHC(O)OR, gdje je R nesupstituirani alifatski C1-6; po izboru:
pri čemu je barem jedan od R2
[image]
ili:
gdje je najmanje jedan od R2 -NHS(O)2R, gdje je R nesupstituirani alifatski C1-6; po izboru:
pri čemu je barem jedan od R2
[image]
ili:
pri čemu je najmanje jedan od R2 -OR, gdje je R:
vodik;
alifatksi C1-6 po izboru supstituiran halogenom, -OH,
[image]
[image]
-C(O)NHC1-4alifatski, -COOH, -C(O)OC1-4alifatski, -CN, -SO2C1-4alifatski, ili
[image]
ili 4-6-eročlani zasićeni monociklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika ili kisika; po izboru:
pri čemu je najmanje jedan od R2 odabran od -OH, -O-CH2-C≡CH,
[image]
[image]
[image]
[image]
[image]
[image]
i
[image]
ili:
pri čemu je najmanje jedan od R2 -P(O)R2, pri čemu je svaki od R neovisno nesupstituirani alifatski C1-6; po izboru:
pri čemu je barem jedan od R2
[image]
ili:
gdje je najmanje jedan od R2 -SR, gdje je R nesupstituirani alifatski C1-6; po izboru:
pri čemu je barem jedan od R2
[image]
po izboru za to:
pri čemu je barem jedan od R2
[image]
ili:
pri čemu je najmanje jedan od R2 -S(O)R, gdje je R nesupstituirani alifatski C1-6; ili:
pri čemu je najmanje jedan od R2 -S(O)2R, gdje je R nesupstituirani alifatski C1-6 ili 3-6-eročlani zasićeni monociklički karbociklički prsten; po izboru:
pri čemu je najmanje jedan od R2 odabran između
[image]
i
[image]
ili:
pri čemu je najmanje jedan od R2 -S(O)(NH)R, gdje je R nesupstituirani alifatski C1-6; po izboru:
pri čemu je barem jedan od R2
[image]
ili:
pri čemu je najmanje jedan od R2 -S(O)2NR2; po izboru:
pri čemu je najmanje jedan od R2 -S(O)2NH2.
6. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je najmanje jedan od R3 alifatski C1-3; i/ili:
gdje X je -O-; i/ili:
gdje je m 1; i/ili:
gdje je p 0; i/ili:
gdje n je 1, 2, 3, 4 ili 5; i/ili:
pri čemu
[image]
je jednostruka veza.
7. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je spoj formule VII
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
n’ je 1 ili 2; i
R2’ je halogen ili alifatski -OC1-3; ili:
gdje je spoj formule VIII
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
prsten B je 5-7-eročlani djelomično nezasićeni heterociklički prsten koji ima 1-2 heteroatoma neovisno odabrana od dušika, kisika ili sumpora, ili prsten B je 5-6-eročlani heteroaromatski prsten koji ima 1-4 heteroatoma neovisno odabrana od dušika, kisika ili sumpora;
n’’ je 0, 1, 2, 3 ili 4; i
R2’ je halogen ili alifatski -OC1-3.
8. Spoj u skladu s patnetnim zahtjevom 7 ili njegova farmaceutski prihvatljiva sol, naznačeno time, da R2' je halogen ili alifatski -OC1-3; ili:
gdje je R2' Cl; ili:
pri čemu je R2’ -OCH3.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 7 ili 8 ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je spoj formule VII-a
[image]
R2’ je Cl.
10. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je spoj formule XI ili XI-a,
[image]
11. Spoj u skladu s patentnim zahtjevom 10 ili njegova farmaceutski prihvatljiva sol, naznačeno time, da R2’ je Cl i svaki od R2 je odabran iz skupine koju čine halogen, -NH2, -CH3, -CF3,
[image]
-CH2CH3,
[image]
[image]
=O, -OH, - COOH,
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
-S(O)2NH2, -OCHF2, -OCF3, -C≡CH, -O-CH2-C≡CH,
[image]
[image]
[image]
[image]
[image]
[image]
i
[image]
12. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je spoj odabran između spojeva prikazanih u tablicama 1, 2 i 2A.
13. Spoj u skladu s patentnim zahtjevom 12 ili njegova farmaceutski prihvatljiva sol, naznačeno time, što je spoj odabran između spojeva
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
i
[image]
14. Spoj su skladu s bilo kojim od patentnih zahtjeva 12 i 13 ili njegova farmaceutski prihvatljiva sol, naznačeno time, da je spoj
[image]
15. Farmaceutski pripravak, naznačeno time, što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14 ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljiv nosač, pomoćno sredstvo ili vehikulum.
16. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14 ili njegova farmaceutski prihvatljiva sol ili njegov farmaceutski pripravak, naznačeno time, da je za uporabu u postupku za liječenje staničnog proliferacijskog poremećaja kod pacijenta, koji uključuje davanje navedenom pacijentu navedenog spoja ili farmaceutskog pripravka.
17. Spoj ili pripravak za uporabu u skladu s patentnim zahtjevom 16, naznačeno time, da navedena uporaba nadalje uključuje određivanje razine ekspresije volframina (WFS1).
18. Spoj ili pripravak za uporabu u skladu s patentnim zahtjevima 16 ili 17, naznačeno time, što je stanični proliferacijski poremećaj karcinom; ili:
pri čemu je stanični proliferacijski poremećaj odabran između karcinoma pluća ne-malih stanica (NSCLC), mijeloma, hepatocelularnog karcinoma (HCC), raka dojke, raka debelog crijeva, raka endometrija, raka jednjaka, raka gušterače, karcinoma bubrežnih stanica i melanoma.
19. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14 ili njegova farmaceutski prihvatljiva sol ili njegov farmaceutski pripravak, za uporabu u postupku za izazivanje ER stresa kod pacijenta kojem je to potrebno, koji postupak se sastoji od davanja navedenog spoja ili pripravka navedenom pacijentu; ili:
spoj prema bilo kojem od zahtjeva 1 do 14, naznačeno time, da se koristi u postupku za induciranje odgovora ne savijenog proteina (UPR) kod pacijenta kojem je to potrebno, a koji postupak se sastoji od davanja navedenom pacijentu navedenog spoja ili pripravka.
20. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14 ili njegova farmaceutski prihvatljiva sol ili njegov farmaceutski pripravak, naznačeno time, da je za uporabu u postupku za izazivanje otpuštanja kalcija iz endoplazmatskog retikuluma (ER) preko navodnog Ca2+ kanala poznatog kao volframin (WFS1) kod pacijenta kojem je to potrebno, koji postupak uključuje davanje navedenom pacijentu navedenog spoja ili pripravka.
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WO2020236834A1 (en) * | 2019-05-20 | 2020-11-26 | Seshadri Raju | Modified z stents for iliac vein stenting |
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TR200400105T4 (tr) | 1999-12-10 | 2004-02-23 | Prizer Products Inc. | Pirrolo [2,3-d] pirimidin bileşikleri |
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