HRP20220039T1 - Aktivatori piruvat kinaze za uporabu u liječenju krvnih poremećaja - Google Patents
Aktivatori piruvat kinaze za uporabu u liječenju krvnih poremećaja Download PDFInfo
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- HRP20220039T1 HRP20220039T1 HRP20220039TT HRP20220039T HRP20220039T1 HR P20220039 T1 HRP20220039 T1 HR P20220039T1 HR P20220039T T HRP20220039T T HR P20220039TT HR P20220039 T HRP20220039 T HR P20220039T HR P20220039 T1 HRP20220039 T1 HR P20220039T1
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- 208000019838 Blood disease Diseases 0.000 title 1
- 102000013009 Pyruvate Kinase Human genes 0.000 title 1
- 108020005115 Pyruvate Kinase Proteins 0.000 title 1
- 239000012190 activator Substances 0.000 title 1
- 208000014951 hematologic disease Diseases 0.000 title 1
- 208000018706 hematopoietic system disease Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 70
- 150000003839 salts Chemical class 0.000 claims 43
- 229910052739 hydrogen Inorganic materials 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 24
- 150000002431 hydrogen Chemical group 0.000 claims 21
- -1 substituted Chemical class 0.000 claims 11
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 9
- 239000000825 pharmaceutical preparation Substances 0.000 claims 9
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical group 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 6
- 208000007502 anemia Diseases 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 208000007475 hemolytic anemia Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000005017 substituted alkenyl 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000035185 Hemolytic Congenital Anemia Diseases 0.000 claims 2
- 206010060893 Hereditary haemolytic anaemia Diseases 0.000 claims 2
- 201000001516 congenital hemolytic anemia Diseases 0.000 claims 2
- 208000024987 familial hemolytic anemia Diseases 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 208000007056 sickle cell anemia Diseases 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000030760 Anaemia of chronic disease Diseases 0.000 claims 1
- 206010014490 Elliptocytosis hereditary Diseases 0.000 claims 1
- 208000001825 Hereditary elliptocytosis Diseases 0.000 claims 1
- 208000000733 Paroxysmal Hemoglobinuria Diseases 0.000 claims 1
- 102100036050 Phosphatidylinositol N-acetylglucosaminyltransferase subunit A Human genes 0.000 claims 1
- 208000002903 Thalassemia Diseases 0.000 claims 1
- 208000004622 abetalipoproteinemia Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000005980 beta thalassemia Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 208000009601 hereditary spherocytosis Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000003045 paroxysmal nocturnal hemoglobinuria Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/14—Ortho-condensed systems
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/495—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
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (39)
1. Spoj, naznačen time, da je predstavljen sljedećom strukturnom formulom:
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
R1 je vodik, opcionalno supstituirani alkil, opcionalno supstituirani haloalkil, opcionalno supstituirani alkenil, opcionalno supstituirani alkinil, opcionalno supstituirani cikloalkil, opcionalno supstituirani heterociklil, opcionalno supstituirani aril, -ORo1, -C(=O)Rc1, ili dušikova zaštitna skupina; pri čemu:
Ro1 je vodik, opcionalno supstituirani alkil, ili kisikova zaštitna skupina;
Rc1 je opcionalno supstituirani alkil ili -N(Rcn)2, pri čemu svaka pojava od Rcn je neovisno vodik, -C1-6 alkil, ili dušikova zaštitna skupina;
svaki od R2 i Q je neovisno opcionalno supstituirani 5-člani ili 6-člani monociklički heteroaril;
svaki od Ra i Rb je neovisno vodik, halogen, -CN, -NO2, -N3, opcionalno supstituirani alkil, -ORo3, -N(Rn1)2, -C(=O)N(Rn1)2, ili -C(=O)Rc2; ili alternativno Ra i Rb mogu biti zajedno s atomom ugljika s kojim su vezani, u svrhu tvorbe opcionalno supstituiranog cikloalkila ili opcionalno supstituiranog heterociklila;
pri čemu:
svaka pojava od Rn1 je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili dušikova zaštitna skupina;
Ro3 je vodik, opcionalno supstituirani -C1-C6 alkil, ili kisikova zaštitna skupina; i
Rc2 je opcionalno supstituirani -C1-C6 alkil; i
svaki od Rj i Rk je neovisno vodik, halogen, -CN, -ORo7, -N(Rn5)2, -N(Rn5)C(=O)Rc5, -C(=O)N(Rn5)2, -C(=O)Rc5, -C(=O)ORo7, -SRjs, -S(=O)2Rjs, -S(=O)Rjs, ili opcionalno supstituirani -C1-C6 alkil; ili alternativno Rj i Rk mogu biti zajedno s atomom ugljika s kojim su vezani, u svrhu tvorbe C=O, opcionalno supstituiranog C1-C6 monocikličkog cikloalkilnog prstena, ili opcionalno supstituiranog C3-C6 monocikličkog heterociklilnog prstena;
pri čemu:
svaka pojava od Rn5je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili dušikova zaštitna skupina, gdje Ro8je vodik, opcionalno supstituirani -C1-C6 alkil, ili kisikova zaštitna skupina;
svaka pojava od Ro7 je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili kisikova zaštitna skupina;
svaka pojava od Rc5 je neovisno opcionalno supstituirani -C1-C6 alkil, i
svaka pojava od Rjs je neovisno opcionalno supstituirani -C1-C6 alkil, opcionalno supstituirani C6-C12 aril, opcionalno supstituirani heteroaril, ili sumporova zaštitna skupina.
2. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je 5-člani ili 6-člani monociklički heteroaril koji je predstavljen s R2, opcionalno supstituiran s Rp na svakom atomu ugljika koji se može supstituirati u prstenu, i opcionalno supstituiran s Rn6 na svakom atomu dušika koji se može supstituirati u prstenu; pri čemu:
svaka pojava od Rp je neovisno vodik, halogen, -CN, -NO2, -N3, opcionalno supstituirani alkil, opcionalno supstituirani alkenil, opcionalno supstituirani alkinil, opcionalno supstituirani cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani heterociklil, opcionalno supstituirani heteroaril, -ORo6, -SRs2, -N(Rn3)2, -C(=O)N(Rn3)2, -N(Rn3)C(=O)Rc4, -C(=O)Rc4, -C(=O)ORo6, -OC(=O)Rc4, -S(=O)Rs2, -S(=O)2Rs2, -S(=O)ORo6, -OS(=O)Rc4, -S(=O)2ORo6, -OS(=O)2Rc4, -S(=O)N(Rn3)2, -S(=O)2N(Rn3)2, -N(Rn3)S(=O)Rs2, -N(Rn3)S(=O)2Rs2, -N(Rn3)C(=O)ORo6, -OC(=O)N(Rn3)2, -N(Rn3)C(=O)N(Rn3)2, -N(Rn3)S(=O)N(Rn3)2, -N(Rn3)S(=O)2N(Rn3)2, -N(Rn3)S(=O)ORo6, -N(Rn3)S(=O)2ORo6, -OS(=O)N(Rn3)2, ili -OS(=O)2N(Rn3)2, ili alternativno dvije pojave od Rp koje su vezane na isti ili susjedne atome ugljika, mogu biti zajedno s atomom/atomima ugljika s kojim/a su vezani, u svrhu tvorbe opcionalno supstituiranog cikloalkila ili heterocikloalkila; pri čemu:
svaka pojava od Rn3je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili dušikova zaštitna skupina;
svaka pojava od Ro6je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili kisikova zaštitna skupina; i
svaka pojava od Rc4je opcionalno supstituirani -C1-C6 alkil;
svaka pojava od Rs2je neovisno opcionalno supstituirani -C1-C6 alkil, ili sumporova zaštitna skupina; i
Rn6 je vodik, opcionalno supstituirani -C1-C6 alkil, ili dušikova zaštitna skupina.
3. Spoj prema bilo kojem od patentnih zahtjeva 1 i 2 ili njegova farmaceutski prihvatljiva sol, naznačen time, da se 5-člani ili 6-člani monociklički heteroaril koji je predstavljen s R2, bira od jednog od sljedećih:
[image]
[image]
gdje:
svaka pojava od Rnc i Rnd je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili dušikova zaštitna skupina; i
p je 0, 1, 2, 3 ili 4, kako dopušta valencija.
4. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da
(a) spoj je predstavljen sljedećom strukturnom formulom:
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu q je 0, 1, 2 ili 3; ili
(b) spoj je predstavljen sljedećom strukturnom formulom:
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu q je 0, 1, 2 ili 3.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da
(a) spoj je predstavljen sljedećom strukturnom formulom:
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu q je 0, 1, 2 ili 3; ili
(b) spoj je predstavljen sljedećom strukturnom formulom:
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu q je 0, 1, 2 ili 3.
6. Spoj prema bilo kojem od patentnih zahtjeva 2 do 4 ili njegova farmaceutski prihvatljiva sol, naznačen time, da svaka pojava od Rp je neovisno vodik, halogen, opcionalno supstituirani C1-4 alkil, -CN, -NO2, -N3, -ORo6, -N(Rn3)2, -C(=O)N(Rn3)2, -C(=O)Rc4, ili -C(=O)ORo6.
7. Spoj prema bilo kojem od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačen time, da
(a) se 5-člani ili 6-člani monociklički heteroaril koji je predstavljen s Q, bira od sljedećih:
[image]
[image]
[image]
gdje:
svaka pojava od Rn je neovisno vodik, halogen, -CN, -NO2, -N3, opcionalno supstituirani alkil, opcionalno supstituirani alkenil, opcionalno supstituirani alkinil, opcionalno supstituirani cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani heterociklil, opcionalno supstituirani heteroaril,
-ORo4, -SRs1, -N(Rn2)2, -C(=O)N(Rn2)2, -N(Rn2)C(=O)Rc3, -C(=O)Rc3, -C(=O)ORo4,
-OC(=O)Rc3, -S(=O)Rs1, -S(=O)2Rs1, -S(=O)ORo4, -OS(=O)Rc3, -S(=O)2ORo4,
-OS(=O)2Rc3, -S(=O)N(Rn2)2, -S(=O)2N(Rn2)2, -N(Rn2)S(=O)Rs1, -N(Rn2)S(=O)2Rs1,
-N(Rn2)C(=O)ORo4, -OC(=O)N(Rn2)2, -N(Rn2)C(=O)N(Rn2)2, -N(Rn2)S(=O)N(Rn2)2,
-N(Rn2)S(=O)2N(Rn2)2, -N(Rn3)S(=O)ORo4, -N(Rn2)S(=O)2ORo4, -OS(=O)N(Rn2)2, ili
-OS(=O)2N(Rn2)2, ili dvije pojave od Rn koje su vezane na isti ili susjedne atome ugljika, mogu biti zajedno s atomima ugljika s kojima su vezani, u svrhu tvorbe opcionalno supstituiranog cikloalkila ili heterocikloalkila; pri čemu:
svaki slučaj Rn2je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili dušikova zaštitna skupina;
svaki slučaj Ro4je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili kisikova zaštitna skupina;
svaki slučaj Rc3je neovisno opcionalno supstituirani -C1-C6 alkil;
svaki slučaj Rs1je neovisno opcionalno supstituirani -C1-C6 alkil, ili sumporova zaštitna skupina;
n je 0, 1, 2 ili 3, kako dopušta valencija; i
svaki od Rna,Rnb iRnd je neovisno vodik, opcionalno supstituirani -C1-C6 alkil, ili dušikova zaštitna skupina;
ili
(b) 5-člani ili 6-člani monociklički heteroaril koji je predstavljen s Q, je
[image]
8. Spoj prema patentnom zahtjevu 7 ili njegova farmaceutski prihvatljiva sol, naznačen time, da svaki slučaj Rn je neovisno vodik, halogen, opcionalno supstituirani C1-4 alkil, -CN, -NO2, -N3, -ORo4, -N(Rn2)2, -C(=O)N(Rn2)2, -C(=O)Rc3, ili -C(=O)ORo4.
9. Spoj prema bilo kojem od prethodnih patentnih zahtjeva ili njegova farmaceutski prihvatljiva sol, naznačen time, da R1 je vodik, ili -C1-C4 alkil, i/ili
time da su svaki Rj i Rk vodik; i/ili
time da su svaki Ra i Rb vodik.
10. Spoj prema patentnom zahtjevu 4 ili zahtjevu 5 ili bilo kojem od patentnih zahtjeva 6 do 9 kada su ovisni o patentnom zahtjevu 4 ili zahtjevu 5, naznačen time, da q je 0 ili 1.
11. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time, da se spoj bira od sljedećih spojeva:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
12. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
13. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
14. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
15. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
16. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
17. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
18. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
19. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
20. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
21. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
22. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
23. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
24. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
25. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
26. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
27. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
28. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
29. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
30. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
31. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
32. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
33. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time, da je spoj predstavljen sljedećom strukturnom formulom:
[image]
34. Farmaceutski pripravak, naznačen time, da sadrži učinkovitu količinu spoja prema bilo kojem od patentnih zahtjeva 1 do 33 ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač.
35. Spoj prema bilo kojem od patentnih zahtjeva 1 do 33 ili njegova farmaceutski prihvatljiva sol; ili farmaceutski pripravak prema patentnom zahtjevu 34, naznačen time, da je za uporabu u postupku liječenja anemije; pri čemu postupak obuhvaća davanje pojedincu učinkovite količine spoja prema bilo kojem od patentnih zahtjeva 1 do 33 ili njegove farmaceutski prihvatljive soli; ili farmaceutskog pripravka prema patentnom zahtjevu 34.
36. Spoj, farmaceutski prihvatljiva sol ili farmaceutski pripravak, za uporabu prema patentnom zahtjevu 35, naznačeni time, da se kod anemije radi o diseritropoetskoj anemiji.
37. Spoj, farmaceutski prihvatljiva sol ili farmaceutski pripravak, za uporabu prema patentnom zahtjevu 35, naznačeni time, da se kod anemije radi o hemolitičkoj anemiji; opcionalno pritom hemolitička anemija je nasljedna i/ili urođena hemolitička anemija, stečena hemolitička anemija, ili anemija kao dio višestruke sustavne bolesti.
38. Spoj prema bilo kojem od patentnih zahtjeva 1 do 33 ili njegova farmaceutski prihvatljiva sol; ili farmaceutski pripravak prema patentnom zahtjevu 34, naznačen time, da je za uporabu u postupku liječenja bolesti srpastih stanica; pri čemu postupak obuhvaća davanje pojedincu učinkovite količine spoja prema bilo kojem od patentnih zahtjeva 1 do 33 ili njegove farmaceutski prihvatljive soli; ili farmaceutskog pripravka prema patentnom zahtjevu 34.
39. Spoj prema bilo kojem od patentnih zahtjeva 1 do 33 ili njegova farmaceutski prihvatljiva sol; ili farmaceutski pripravak prema patentnom zahtjevu 34, naznačen time, da je za uporabu u postupku liječenja talasemije, poželjno beta-talasemije, nasljedne sferocitoze, nasljedne eliptocitoze, abetalipoproteinemije ili Bassen-Kornzweigovog sindroma, bolesti srpastih stanica, paroksizmalne noćne hemoglobinurije, stečene hemolitičke anemije, ili anemije kod kroničnih bolesti; pri čemu postupak obuhvaća davanje pojedincu učinkovite količine spoja prema bilo kojem od patentnih zahtjeva 1 do 33 ili njegove farmaceutski prihvatljive soli; ili farmaceutskog pripravka prema patentnom zahtjevu 34.
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| EP18779068.8A EP3668513B1 (en) | 2017-08-15 | 2018-08-15 | Pyruvate kinase activators for use in treating blood disorders |
| PCT/US2018/000128 WO2019035864A1 (en) | 2017-08-15 | 2018-08-15 | PYRUVATE KINASE ACTIVATORS FOR USE IN THE TREATMENT OF BLOOD DISORDERS |
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| JP7450610B2 (ja) | 2018-09-19 | 2024-03-15 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | ピルビン酸キナーゼｒの活性化 |
| US20200129485A1 (en) | 2018-09-19 | 2020-04-30 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| WO2020167976A1 (en) * | 2019-02-13 | 2020-08-20 | Agios Pharmaceuticals, Inc. | Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders |
| KR20220025814A (ko) * | 2019-06-26 | 2022-03-03 | 닛산 가가쿠 가부시키가이샤 | 전하 수송성 바니시 |
| CN116249531A (zh) * | 2020-07-21 | 2023-06-09 | 密执安大学评议会 | 用于激活丙酮酸激酶的组合物和方法 |
| CN112490502B (zh) * | 2020-12-04 | 2022-01-21 | 广州天赐高新材料股份有限公司 | 一种电解液及锂二次电池 |
| WO2022170200A1 (en) | 2021-02-08 | 2022-08-11 | Global Blood Therapeutics, Inc. | 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease |
| WO2023052783A1 (en) * | 2021-09-30 | 2023-04-06 | Sitryx Therapeutics Limited | Novel compounds |
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