UA79066C2 - Transdominant inhibitory kinase h-sgk in which lysine is substituted in the 127 position by arginine, and its use for preparation the remedy - Google Patents
Transdominant inhibitory kinase h-sgk in which lysine is substituted in the 127 position by arginine, and its use for preparation the remedy Download PDFInfo
- Publication number
- UA79066C2 UA79066C2 UA2001117896A UA2001117896A UA79066C2 UA 79066 C2 UA79066 C2 UA 79066C2 UA 2001117896 A UA2001117896 A UA 2001117896A UA 2001117896 A UA2001117896 A UA 2001117896A UA 79066 C2 UA79066 C2 UA 79066C2
- Authority
- UA
- Ukraine
- Prior art keywords
- kinase
- expression
- arginine
- lysine
- disease
- Prior art date
Links
- 230000002401 inhibitory effect Effects 0.000 title claims description 9
- 239000004475 Arginine Substances 0.000 title claims description 4
- 239000004472 Lysine Substances 0.000 title claims description 4
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 title claims description 4
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 title claims description 4
- 238000002360 preparation method Methods 0.000 title claims description 4
- 108091000080 Phosphotransferase Proteins 0.000 title abstract description 24
- 102000020233 phosphotransferase Human genes 0.000 title abstract description 24
- 230000003176 fibrotic effect Effects 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 230000000694 effects Effects 0.000 claims description 7
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 208000011231 Crohn disease Diseases 0.000 claims description 6
- 206010033645 Pancreatitis Diseases 0.000 claims description 6
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 6
- 208000005069 pulmonary fibrosis Diseases 0.000 claims description 6
- 206010006458 Bronchitis chronic Diseases 0.000 claims description 5
- 206010006451 bronchitis Diseases 0.000 claims description 5
- 208000007451 chronic bronchitis Diseases 0.000 claims description 5
- 102000001253 Protein Kinase Human genes 0.000 claims description 3
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims description 3
- 108060006633 protein kinase Proteins 0.000 claims description 3
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 claims description 2
- 206010067953 Radiation fibrosis Diseases 0.000 claims description 2
- 206010039710 Scleroderma Diseases 0.000 claims description 2
- 208000037849 arterial hypertension Diseases 0.000 claims description 2
- 229940126601 medicinal product Drugs 0.000 claims description 2
- 102000003837 Epithelial Sodium Channels Human genes 0.000 claims 1
- 108090000140 Epithelial Sodium Channels Proteins 0.000 claims 1
- 102000003673 Symporters Human genes 0.000 claims 1
- 108090000088 Symporters Proteins 0.000 claims 1
- 230000014509 gene expression Effects 0.000 abstract description 27
- 239000003112 inhibitor Substances 0.000 abstract description 10
- 239000012190 activator Substances 0.000 abstract description 7
- 239000003814 drug Substances 0.000 abstract description 6
- 230000001105 regulatory effect Effects 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 description 14
- 230000000638 stimulation Effects 0.000 description 14
- LLEJIEBFSOEYIV-UHFFFAOYSA-N chelerythrine Chemical compound C1=C2OCOC2=CC2=CC=C3C4=CC=C(OC)C(OC)=C4C=[N+](C)C3=C21 LLEJIEBFSOEYIV-UHFFFAOYSA-N 0.000 description 12
- 210000000287 oocyte Anatomy 0.000 description 11
- 230000004186 co-expression Effects 0.000 description 10
- 206010016654 Fibrosis Diseases 0.000 description 9
- 210000001519 tissue Anatomy 0.000 description 9
- 102000004954 Biglycan Human genes 0.000 description 8
- 108090001138 Biglycan Proteins 0.000 description 8
- 229960003883 furosemide Drugs 0.000 description 8
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 description 8
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 7
- 229940043355 kinase inhibitor Drugs 0.000 description 7
- 210000004185 liver Anatomy 0.000 description 7
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 7
- HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 description 7
- RATMHCJTVBHJSU-UHFFFAOYSA-N Dihydrochelerythrine Natural products C1=C2OCOC2=CC2=C(N(C)C(O)C=3C4=CC=C(C=3OC)OC)C4=CC=C21 RATMHCJTVBHJSU-UHFFFAOYSA-N 0.000 description 6
- HKSZLNNOFSGOKW-UHFFFAOYSA-N ent-staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(C)O1 HKSZLNNOFSGOKW-UHFFFAOYSA-N 0.000 description 6
- CGPUWJWCVCFERF-UHFFFAOYSA-N staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(OC)O1 CGPUWJWCVCFERF-UHFFFAOYSA-N 0.000 description 6
- 108091006146 Channels Proteins 0.000 description 5
- 230000007882 cirrhosis Effects 0.000 description 5
- 238000002474 experimental method Methods 0.000 description 5
- 230000035515 penetration Effects 0.000 description 5
- 206010003210 Arteriosclerosis Diseases 0.000 description 4
- 208000011775 arteriosclerosis disease Diseases 0.000 description 4
- 206010012601 diabetes mellitus Diseases 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 230000004761 fibrosis Effects 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- 210000003734 kidney Anatomy 0.000 description 4
- 206010001497 Agitation Diseases 0.000 description 3
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 230000004913 activation Effects 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 210000004556 brain Anatomy 0.000 description 3
- 238000009396 hybridization Methods 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 210000000496 pancreas Anatomy 0.000 description 3
- QKNYBSVHEMOAJP-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol;hydron;chloride Chemical compound Cl.OCC(N)(CO)CO QKNYBSVHEMOAJP-UHFFFAOYSA-N 0.000 description 2
- ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 description 2
- 108060003393 Granulin Proteins 0.000 description 2
- WZUVPPKBWHMQCE-UHFFFAOYSA-N Haematoxylin Chemical compound C12=CC(O)=C(O)C=C2CC2(O)C1C1=CC=C(O)C(O)=C1OC2 WZUVPPKBWHMQCE-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 2
- 206010033799 Paralysis Diseases 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 230000008499 blood brain barrier function Effects 0.000 description 2
- 210000001218 blood-brain barrier Anatomy 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 230000003197 catalytic effect Effects 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 230000004907 flux Effects 0.000 description 2
- 238000011534 incubation Methods 0.000 description 2
- 230000035772 mutation Effects 0.000 description 2
- 230000001537 neural effect Effects 0.000 description 2
- 210000002569 neuron Anatomy 0.000 description 2
- 239000012188 paraffin wax Substances 0.000 description 2
- 238000003752 polymerase chain reaction Methods 0.000 description 2
- 229910052700 potassium Inorganic materials 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 239000000523 sample Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 230000004936 stimulating effect Effects 0.000 description 2
- WFCSWCVEJLETKA-UHFFFAOYSA-N 2-piperazin-1-ylethanol Chemical compound OCCN1CCNCC1 WFCSWCVEJLETKA-UHFFFAOYSA-N 0.000 description 1
- DGOSGFYDFDYMCW-OEFRVDPMSA-N 4alpha-phorbol 12,13-didecanoate Chemical compound C([C@@]1(O)C(=O)C(C)=C[C@H]1[C@@]1(O)[C@H](C)[C@H]2OC(=O)CCCCCCCCC)C(CO)=C[C@H]1[C@H]1[C@]2(OC(=O)CCCCCCCCC)C1(C)C DGOSGFYDFDYMCW-OEFRVDPMSA-N 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- 108020005544 Antisense RNA Proteins 0.000 description 1
- 241000972773 Aulopiformes Species 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 1
- SHIBSTMRCDJXLN-UHFFFAOYSA-N Digoxigenin Natural products C1CC(C2C(C3(C)CCC(O)CC3CC2)CC2O)(O)C2(C)C1C1=CC(=O)OC1 SHIBSTMRCDJXLN-UHFFFAOYSA-N 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 239000004677 Nylon Substances 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 108020002230 Pancreatic Ribonuclease Proteins 0.000 description 1
- 102000005891 Pancreatic ribonuclease Human genes 0.000 description 1
- 229930040373 Paraformaldehyde Natural products 0.000 description 1
- 108090000315 Protein Kinase C Proteins 0.000 description 1
- 102000003923 Protein Kinase C Human genes 0.000 description 1
- 239000013614 RNA sample Substances 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 description 1
- 108010071390 Serum Albumin Proteins 0.000 description 1
- 102000007562 Serum Albumin Human genes 0.000 description 1
- 108010052164 Sodium Channels Proteins 0.000 description 1
- 102000018674 Sodium Channels Human genes 0.000 description 1
- 108091093130 Toxic Small RNA Proteins 0.000 description 1
- 102000009618 Transforming Growth Factors Human genes 0.000 description 1
- 108010009583 Transforming Growth Factors Proteins 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 238000000376 autoradiography Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 229960004064 bumetanide Drugs 0.000 description 1
- MAEIEVLCKWDQJH-UHFFFAOYSA-N bumetanide Chemical compound CCCCNC1=CC(C(O)=O)=CC(S(N)(=O)=O)=C1OC1=CC=CC=C1 MAEIEVLCKWDQJH-UHFFFAOYSA-N 0.000 description 1
- 239000001110 calcium chloride Substances 0.000 description 1
- 229910001628 calcium chloride Inorganic materials 0.000 description 1
- 244000309466 calf Species 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 238000006555 catalytic reaction Methods 0.000 description 1
- 230000001364 causal effect Effects 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- 230000000295 complement effect Effects 0.000 description 1
- 239000003184 complementary RNA Substances 0.000 description 1
- 210000002808 connective tissue Anatomy 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 229960000633 dextran sulfate Drugs 0.000 description 1
- 208000033679 diabetic kidney disease Diseases 0.000 description 1
- QONQRTHLHBTMGP-UHFFFAOYSA-N digitoxigenin Natural products CC12CCC(C3(CCC(O)CC3CC3)C)C3C11OC1CC2C1=CC(=O)OC1 QONQRTHLHBTMGP-UHFFFAOYSA-N 0.000 description 1
- SHIBSTMRCDJXLN-KCZCNTNESA-N digoxigenin Chemical compound C1([C@@H]2[C@@]3([C@@](CC2)(O)[C@H]2[C@@H]([C@@]4(C)CC[C@H](O)C[C@H]4CC2)C[C@H]3O)C)=CC(=O)OC1 SHIBSTMRCDJXLN-KCZCNTNESA-N 0.000 description 1
- 238000002224 dissection Methods 0.000 description 1
- VHJLVAABSRFDPM-QWWZWVQMSA-N dithiothreitol Chemical compound SC[C@@H](O)[C@H](O)CS VHJLVAABSRFDPM-QWWZWVQMSA-N 0.000 description 1
- 238000001962 electrophoresis Methods 0.000 description 1
- 210000001842 enterocyte Anatomy 0.000 description 1
- 230000007515 enzymatic degradation Effects 0.000 description 1
- YQGOJNYOYNNSMM-UHFFFAOYSA-N eosin Chemical compound [Na+].OC(=O)C1=CC=CC=C1C1=C2C=C(Br)C(=O)C(Br)=C2OC2=C(Br)C(O)=C(Br)C=C21 YQGOJNYOYNNSMM-UHFFFAOYSA-N 0.000 description 1
- 230000001037 epileptic effect Effects 0.000 description 1
- 239000012894 fetal calf serum Substances 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 230000002102 hyperpolarization Effects 0.000 description 1
- 230000036543 hypotension Effects 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- PGHMRUGBZOYCAA-ADZNBVRBSA-N ionomycin Chemical compound O1[C@H](C[C@H](O)[C@H](C)[C@H](O)[C@H](C)/C=C/C[C@@H](C)C[C@@H](C)C(/O)=C/C(=O)[C@@H](C)C[C@@H](C)C[C@@H](CCC(O)=O)C)CC[C@@]1(C)[C@@H]1O[C@](C)([C@@H](C)O)CC1 PGHMRUGBZOYCAA-ADZNBVRBSA-N 0.000 description 1
- PGHMRUGBZOYCAA-UHFFFAOYSA-N ionomycin Natural products O1C(CC(O)C(C)C(O)C(C)C=CCC(C)CC(C)C(O)=CC(=O)C(C)CC(C)CC(CCC(O)=O)C)CCC1(C)C1OC(C)(C(C)O)CC1 PGHMRUGBZOYCAA-UHFFFAOYSA-N 0.000 description 1
- 239000002555 ionophore Substances 0.000 description 1
- 230000000236 ionophoric effect Effects 0.000 description 1
- 210000001039 kidney glomerulus Anatomy 0.000 description 1
- 210000001865 kupffer cell Anatomy 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 229910001629 magnesium chloride Inorganic materials 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 210000005087 mononuclear cell Anatomy 0.000 description 1
- 230000008587 neuronal excitability Effects 0.000 description 1
- 229920001778 nylon Polymers 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 229920002866 paraformaldehyde Polymers 0.000 description 1
- PHEDXBVPIONUQT-RGYGYFBISA-N phorbol 13-acetate 12-myristate Chemical compound C([C@]1(O)C(=O)C(C)=C[C@H]1[C@@]1(O)[C@H](C)[C@H]2OC(=O)CCCCCCCCCCCCC)C(CO)=C[C@H]1[C@H]1[C@]2(OC(C)=O)C1(C)C PHEDXBVPIONUQT-RGYGYFBISA-N 0.000 description 1
- 239000002644 phorbol ester Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 230000022532 regulation of transcription, DNA-dependent Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 235000019515 salmon Nutrition 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000011121 sodium hydroxide Nutrition 0.000 description 1
- 239000012064 sodium phosphate buffer Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 210000005239 tubule Anatomy 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
-
- 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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/005—Enzyme inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19917990A DE19917990A1 (de) | 1999-04-20 | 1999-04-20 | Arzneimittel enthaltend Hemmstoffe der zellvolumenregulierten humanen Kinase h-sgk |
| PCT/EP2000/003578 WO2000062781A1 (de) | 1999-04-20 | 2000-04-19 | Arzneimittel enthaltend hemmstoffe der zellvolumenregulierten humanen kinase h-sgk |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA79066C2 true UA79066C2 (en) | 2007-05-25 |
Family
ID=7905297
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UA2001117896A UA79066C2 (en) | 1999-04-20 | 2000-04-19 | Transdominant inhibitory kinase h-sgk in which lysine is substituted in the 127 position by arginine, and its use for preparation the remedy |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP1171131A1 (es) |
| JP (1) | JP2002542196A (es) |
| KR (1) | KR100718900B1 (es) |
| CN (1) | CN1351496A (es) |
| AU (1) | AU779941B2 (es) |
| BR (1) | BR0009914A (es) |
| CA (1) | CA2369078A1 (es) |
| CZ (1) | CZ20013778A3 (es) |
| DE (1) | DE19917990A1 (es) |
| HU (1) | HUP0200819A3 (es) |
| MX (1) | MXPA01010588A (es) |
| NO (1) | NO20015054L (es) |
| PL (1) | PL198427B1 (es) |
| RU (1) | RU2288718C9 (es) |
| SK (1) | SK14972001A3 (es) |
| UA (1) | UA79066C2 (es) |
| WO (1) | WO2000062781A1 (es) |
| ZA (1) | ZA200108610B (es) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10042137A1 (de) * | 2000-08-28 | 2002-03-14 | Florian Lang | sgk2 und sgk3 als diagnostische und therapeutische Targets |
| DE10113876A1 (de) * | 2001-03-21 | 2002-09-26 | Eberhard Karls Uni Medizinisch | Quantitative diagnostische Analyse der Hypertonie |
| CA2449794A1 (en) | 2001-04-27 | 2002-11-07 | Cold Spring Harbor Laboratory | Alleviation of the memory deficits and memory components of psychiatric dysfunctions by altering atypical pkm activity |
| DE10149393A1 (de) * | 2001-09-28 | 2003-04-24 | Florian Lang | sgk1 als diagnostisches und therapeutisches target |
| DE10225844A1 (de) * | 2002-06-04 | 2003-12-18 | Lang Florian | sgk und nedd als diagnostische und therapeutische targets |
| DE10305212A1 (de) * | 2003-02-07 | 2004-08-19 | Florian Prof. Dr.med. Lang | Verwendung der sgk-Genfamilie zur Diagnose und zur Therapie von Katarakt und Glaukom |
| WO2004079003A1 (de) * | 2003-03-03 | 2004-09-16 | Florian Lang | Sgk1 als diagnostisches und therapeutisches target |
| WO2004084889A1 (en) * | 2003-03-28 | 2004-10-07 | Pfizer Inc. | Use of protein kinase c inhibitor for suppressing sustained slow postsynaptic excitation (sspe) of enteric neurons |
| DE10346913A1 (de) * | 2003-10-09 | 2005-05-04 | Merck Patent Gmbh | Acylhydrazonderivate |
| WO2005084702A1 (ja) * | 2004-03-02 | 2005-09-15 | Hokkaido Technology Licensing Office Co., Ltd. | 臓器線維症予防・治療剤 |
| WO2005094796A2 (en) * | 2004-03-11 | 2005-10-13 | Merck Patent Gmbh | Methods for interfering with fibrosis |
| US20070191326A1 (en) * | 2004-03-11 | 2007-08-16 | Florian Lang | Methods for modulating glutamate receptors for treating neuropsychiatric disorders comprising the use of modulators of serum and glucocorticoid inducible kinases |
| US20090136920A1 (en) * | 2004-04-30 | 2009-05-28 | Stefan Golz | Diagnostics and therapeutics for diseases associated with serum/glucocorticoid regulated kinase 1 (sgk1) |
| WO2005118832A2 (en) * | 2004-06-01 | 2005-12-15 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with serum/glucocorticoid regulated kinase-like protein (sgkl) |
| DE102004030987A1 (de) * | 2004-06-26 | 2006-01-12 | Merck Patent Gmbh | Ortho-substituierte (3-Hydroxyphenyl)-essigsäure-benzyliden-hydrazide |
| MX2007001155A (es) * | 2004-07-29 | 2007-08-14 | Creabilis Therapeutics Spa | Uso de inhibidores de k-252a y de quinasa para la prevencion o el tratamiento de patologias asociadas con hmgb1. |
| DE102005001053A1 (de) * | 2005-01-07 | 2006-07-20 | Merck Patent Gmbh | Quadratsäurederivate |
| DE102005015255A1 (de) * | 2005-04-04 | 2006-10-05 | Merck Patent Gmbh | Acylhydrazide |
| DE102005035742A1 (de) * | 2005-07-29 | 2007-02-01 | Merck Patent Gmbh | Quadratsäurederivate II |
| DE102005039541A1 (de) * | 2005-08-22 | 2007-03-22 | Merck Patent Gmbh | 3-Oxo-indazol-quadratsäurederivate |
| DE102007002717A1 (de) | 2007-01-18 | 2008-07-24 | Merck Patent Gmbh | Heterocyclische Indazolderivate |
| DE102007022565A1 (de) | 2007-05-14 | 2008-11-20 | Merck Patent Gmbh | Heterocyclische Indazolderivate |
| EP2014651A1 (en) * | 2007-07-12 | 2009-01-14 | Exonhit Therapeutics SA | Compounds and methods for modulating Rho GTPases |
| DE102008010363A1 (de) | 2008-02-18 | 2009-08-20 | Lang, Florian, Prof. Dr.med. | Sgk1 als therapeutisches und diagnostisches Target für karzinomatöse Erkrankungen |
| DE102008010362A1 (de) | 2008-02-18 | 2009-08-20 | Florian Prof. Dr. Lang | Sgk1 als therapeutisches und diagnostisches Target für virale Erkrankungen |
| DE102008010361A1 (de) | 2008-02-18 | 2009-08-20 | Merck Patent Gmbh | sgk1-Inhibitoren zur Prophylaxe und/oder Therapie von viralen Erkrankungen und/oder Karzinomen |
| DE102008029072A1 (de) * | 2008-06-10 | 2009-12-17 | Lang, Florian, Prof. Dr.med. | Sgk3 als therapeutisches und diagnostisches Target für Alterserkrankungen |
| DE102008038222A1 (de) | 2008-08-18 | 2010-02-25 | Merck Patent Gmbh | Indazol-5-carbonsäurehydrazid-derivate |
| DE102008038220A1 (de) | 2008-08-18 | 2010-02-25 | Merck Patent Gmbh | Oxadiazolderivate |
| DE102008038221A1 (de) | 2008-08-18 | 2010-02-25 | Merck Patent Gmbh | 7-Azaindolderivate |
| DE102008059133A1 (de) | 2008-11-26 | 2010-05-27 | Merck Patent Gmbh | Difluorphenyl-diacylhydrazid-derivate |
| WO2012064981A2 (en) * | 2010-11-10 | 2012-05-18 | National Jewish Health | Methods to test allergic conditions |
| CN107875153A (zh) * | 2017-11-16 | 2018-04-06 | 上海壹志医药科技有限公司 | 去甲白屈菜红碱的药物用途 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5373501A (en) * | 1976-12-11 | 1978-06-30 | Kitasato Inst | Novel antibiotics amm2282 and process for preparing same |
| US5242397A (en) * | 1989-06-20 | 1993-09-07 | Cedars-Sinai Medical Center | Catheter device and method of use for intramural delivery of protein kinase C and tyrosine protein kinase inhibitors to prevent restenosis after balloon angioplasty |
| US5137912A (en) * | 1991-01-28 | 1992-08-11 | National Science Council Of Republic Of China | Chelerythrine inhibits platelet aggregation--a potential anti-aggregation drug |
| GB9325395D0 (en) * | 1993-12-11 | 1994-02-16 | Ciba Geigy Ag | Compositions |
| US5874464A (en) * | 1995-01-13 | 1999-02-23 | The United States Of America As Represented By The Department Of Health And Human Services | Conformationally constrained diacylglycerol analogues |
| AU6888196A (en) * | 1995-08-11 | 1997-03-12 | Yale University | Glycosylated indolocarbazole synthesis |
| PT906268E (pt) * | 1996-05-30 | 2002-05-31 | Aventis Pharma Inc | Fluorenonas com substituicao alquiloxiamino e sua utilizacao como inibidores da proteina quinase c |
| EP0887081B1 (en) * | 1997-06-27 | 2003-04-23 | Smithkline Beecham Corporation | Human serum glucocorticoid regulated kinase, a target for chronic renal disease and diabetic nephropathy |
| EP0889127A1 (en) * | 1997-07-01 | 1999-01-07 | Smithkline Beecham Corporation | Serine/threonine protein kinase (H-SGK2) |
| CO4940430A1 (es) * | 1997-07-07 | 2000-07-24 | Novartis Ag | Compuestos policiclicos que contienen estaurosporina hidrogenada con propiedades farmacologicas convenientes y un efecto inhibidor sobre el crecimiento de las celulas tumorales |
-
1999
- 1999-04-20 DE DE19917990A patent/DE19917990A1/de not_active Ceased
-
2000
- 2000-04-19 JP JP2000611917A patent/JP2002542196A/ja active Pending
- 2000-04-19 CZ CZ20013778A patent/CZ20013778A3/cs unknown
- 2000-04-19 PL PL352547A patent/PL198427B1/pl unknown
- 2000-04-19 WO PCT/EP2000/003578 patent/WO2000062781A1/de not_active Application Discontinuation
- 2000-04-19 CN CN00807959A patent/CN1351496A/zh active Pending
- 2000-04-19 HU HU0200819A patent/HUP0200819A3/hu unknown
- 2000-04-19 KR KR1020017013336A patent/KR100718900B1/ko not_active IP Right Cessation
- 2000-04-19 UA UA2001117896A patent/UA79066C2/uk unknown
- 2000-04-19 MX MXPA01010588A patent/MXPA01010588A/es not_active Application Discontinuation
- 2000-04-19 AU AU42972/00A patent/AU779941B2/en not_active Ceased
- 2000-04-19 SK SK1497-2001A patent/SK14972001A3/sk unknown
- 2000-04-19 RU RU2001131351/15A patent/RU2288718C9/ru not_active IP Right Cessation
- 2000-04-19 BR BR0009914-7A patent/BR0009914A/pt not_active Application Discontinuation
- 2000-04-19 CA CA002369078A patent/CA2369078A1/en not_active Abandoned
- 2000-04-19 EP EP00922655A patent/EP1171131A1/de not_active Withdrawn
-
2001
- 2001-10-17 NO NO20015054A patent/NO20015054L/no not_active Application Discontinuation
- 2001-10-19 ZA ZA200108610A patent/ZA200108610B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2002542196A (ja) | 2002-12-10 |
| WO2000062781A1 (de) | 2000-10-26 |
| HUP0200819A3 (en) | 2009-08-28 |
| DE19917990A1 (de) | 2000-11-02 |
| PL198427B1 (pl) | 2008-06-30 |
| PL352547A1 (en) | 2003-08-25 |
| CN1351496A (zh) | 2002-05-29 |
| NO20015054D0 (no) | 2001-10-17 |
| RU2288718C2 (ru) | 2006-12-10 |
| KR20020012172A (ko) | 2002-02-15 |
| SK14972001A3 (sk) | 2002-06-04 |
| KR100718900B1 (ko) | 2007-05-17 |
| HUP0200819A2 (hu) | 2002-07-29 |
| AU4297200A (en) | 2000-11-02 |
| ZA200108610B (en) | 2002-01-02 |
| NO20015054L (no) | 2001-12-14 |
| CA2369078A1 (en) | 2000-10-26 |
| EP1171131A1 (de) | 2002-01-16 |
| CZ20013778A3 (cs) | 2002-06-12 |
| MXPA01010588A (es) | 2004-09-06 |
| BR0009914A (pt) | 2002-01-08 |
| AU779941B2 (en) | 2005-02-17 |
| RU2288718C9 (ru) | 2008-04-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| UA79066C2 (en) | Transdominant inhibitory kinase h-sgk in which lysine is substituted in the 127 position by arginine, and its use for preparation the remedy | |
| CA2126083C (en) | Use of app modulators for the manufacture of a medicament for the treatment of amyloidosis | |
| Lanoue et al. | Limb, genital, CNS, and facial malformations result from gene/environment‐induced cholesterol deficiency: further evidence for a link to sonic hedgehog | |
| Shtifman et al. | Amyloid-β protein impairs Ca2+ release and contractility in skeletal muscle | |
| US9382313B2 (en) | Modulation of synaptic maintenance | |
| Origlia et al. | Aβ-dependent Inhibition of LTP in different intracortical circuits of the visual cortex: The role of RAGE | |
| EP2976094B1 (en) | Methods of treating metabolic disorders | |
| O'Leary et al. | Enhanced long term potentiation and decreased AMPA receptor desensitization in the acute period following a single kainate induced early life seizure | |
| KR20030031466A (ko) | 포유동물 세포 증식을 조절하기 위한 ａ２ｂ 아데노신수용체 길항 물질의 동정 및 사용 방법 | |
| CA2320717C (en) | Method for the treatment of diseases or disorders of the inner ear | |
| Prieur et al. | Effects of adrenal steroid hormones on mitochondrial maturation during the late fetal period | |
| US20050064501A1 (en) | Medicaments comprising inhibitors of the cell volume-regulated human kinase h-sgk | |
| Kawao et al. | Tmem119 is involved in bone anabolic effects of PTH through enhanced osteoblastic bone formation in mice | |
| EP0782573B1 (en) | Brefeldin a and analogs to improved synaptic transmission | |
| JPWO2007000884A1 (ja) | 骨・関節疾患の予防・治療剤およびそのスクリーニング方法 | |
| US20040115195A1 (en) | Pharmaceutical compositions and methods of using secreted frizzled related protein | |
| De Deyn et al. | Effects of α-keto-δ-guanidinovaleric acid on inhibitory amino acid responses on mouse neurons in cell culture | |
| Rama et al. | The MUPP1–SynGAPα protein complex does not mediate activity-induced LTP | |
| Poiani et al. | Effect of glucocorticoids on collagen accumulation in pulmonary vascular remodeling in the rat. | |
| Guo et al. | Bone marrow mesenchymal stem cells (BMSC) from exosome with high miR-184 level ameliorates sepsis | |
| EP4085972A1 (en) | Amp-activated protein kinase inhibitors for use in the treatment of ptsd in a subject | |
| WO2024164318A1 (zh) | Gch1抑制剂在制备用于预防和治疗听力损伤的药物中的用途 | |
| Shore et al. | The paradoxical effects of K+ channel gain-of-function are mediated by GABAergic neuron hypoexcitability and hyperconnectivity | |
| Wang et al. | Overexpression of synaptic vesicle protein 2A inhibits seizures and amygdaloid electroencephalogram activity in pilocarpine-induced pharmacoresistant epileptic rats | |
| EP3747468A1 (en) | Therapeutic agent for frontotemporal lobar degeneration, method for screening therapeutic agent for frontotemporal lobar degeneration and method for treating frontotemporal lobar degeneration |