HRP20120078T1 - Pirazolinski spojevi kao antagonisti mineralokortikoidnih receptora - Google Patents
Pirazolinski spojevi kao antagonisti mineralokortikoidnih receptora Download PDFInfo
- Publication number
- HRP20120078T1 HRP20120078T1 HR20120078T HRP20120078T HRP20120078T1 HR P20120078 T1 HRP20120078 T1 HR P20120078T1 HR 20120078 T HR20120078 T HR 20120078T HR P20120078 T HRP20120078 T HR P20120078T HR P20120078 T1 HRP20120078 T1 HR P20120078T1
- Authority
- HR
- Croatia
- Prior art keywords
- group
- alkyl
- cyclopentyl
- benzo
- tetrahydro
- Prior art date
Links
- 229940083712 aldosterone antagonist Drugs 0.000 title 1
- 239000002394 mineralocorticoid antagonist Substances 0.000 title 1
- 150000003219 pyrazolines Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 29
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 24
- 239000001257 hydrogen Substances 0.000 claims abstract 24
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 14
- 150000003839 salts Chemical class 0.000 claims abstract 10
- 229910052801 chlorine Inorganic materials 0.000 claims abstract 9
- 239000000460 chlorine Substances 0.000 claims abstract 9
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims abstract 9
- 229910052731 fluorine Inorganic materials 0.000 claims abstract 9
- 239000011737 fluorine Chemical group 0.000 claims abstract 9
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims abstract 8
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims abstract 8
- -1 cyano, hydroxy, carboxy, methyl Chemical group 0.000 claims abstract 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 6
- 125000001424 substituent group Chemical group 0.000 claims abstract 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims abstract 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract 4
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 claims abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 4
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims abstract 3
- 229910052736 halogen Inorganic materials 0.000 claims abstract 3
- 150000002367 halogens Chemical group 0.000 claims abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims abstract 2
- 125000004218 chloromethyl group Chemical group [H]C([H])(Cl)* 0.000 claims abstract 2
- 125000004772 dichloromethyl group Chemical group [H]C(Cl)(Cl)* 0.000 claims abstract 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims abstract 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims abstract 2
- 150000002431 hydrogen Chemical class 0.000 claims abstract 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims abstract 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- XNULRSOGWPFPBL-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C12CCC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1CCCC1 XNULRSOGWPFPBL-UHFFFAOYSA-N 0.000 claims 2
- DIXPGEVTBJXMRW-UHFFFAOYSA-N 2-(4-cyano-3-methoxyphenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C1=C(C#N)C(OC)=CC(N2C(C3C(C4=CC=C(C=C4CC3)C(O)=O)=N2)C2CCCC2)=C1 DIXPGEVTBJXMRW-UHFFFAOYSA-N 0.000 claims 2
- MLSLCRTVTQJOGF-UHFFFAOYSA-N 2-(4-cyano-3-methylphenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C1=C(C#N)C(C)=CC(N2C(C3C(C4=CC=C(C=C4CC3)C(O)=O)=N2)C2CCCC2)=C1 MLSLCRTVTQJOGF-UHFFFAOYSA-N 0.000 claims 2
- 239000002876 beta blocker Substances 0.000 claims 2
- 229940097320 beta blocking agent Drugs 0.000 claims 2
- ABRSQONXUKMPNK-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-(4-fluorophenyl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C12CCC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1=CC=C(F)C=C1 ABRSQONXUKMPNK-UHFFFAOYSA-N 0.000 claims 1
- ICXQTNPFKOHPPM-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-(4-fluorophenyl)-n-(2-methylsulfonylethyl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxamide Chemical compound C12CCC3=CC(C(=O)NCCS(=O)(=O)C)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1=CC=C(F)C=C1 ICXQTNPFKOHPPM-UHFFFAOYSA-N 0.000 claims 1
- KUWNMBQXHAXMMP-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-(5-methylfuran-2-yl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound O1C(C)=CC=C1C1N(C=2C=C(Cl)C(C#N)=CC=2)N=C2C3=CC=C(C(O)=O)C=C3CCC21 KUWNMBQXHAXMMP-UHFFFAOYSA-N 0.000 claims 1
- YWQXDRZXKRBIBO-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-(5-methylfuran-2-yl)-n-(2-methylsulfonylethyl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxamide Chemical compound O1C(C)=CC=C1C1N(C=2C=C(Cl)C(C#N)=CC=2)N=C2C3=CC=C(C(=O)NCCS(C)(=O)=O)C=C3CCC21 YWQXDRZXKRBIBO-UHFFFAOYSA-N 0.000 claims 1
- OHABSNPTOQCUGY-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-(cyclopenten-1-yl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C12CCC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1=CCCC1 OHABSNPTOQCUGY-UHFFFAOYSA-N 0.000 claims 1
- RQYBCTCZSWIXNY-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-(cyclopenten-1-yl)-3a,4-dihydro-3h-chromeno[4,3-c]pyrazole-7-carboxylic acid Chemical compound C12COC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1=CCCC1 RQYBCTCZSWIXNY-UHFFFAOYSA-N 0.000 claims 1
- JZMZZNBXXUCHGC-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-(furan-3-yl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C12CCC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C=1C=COC=1 JZMZZNBXXUCHGC-UHFFFAOYSA-N 0.000 claims 1
- CRYDENMXDBTLTA-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-cyclobutyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C12CCC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1CCC1 CRYDENMXDBTLTA-UHFFFAOYSA-N 0.000 claims 1
- PHZPYPOXYQPPFG-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3a,4-dihydro-3h-chromeno[4,3-c]pyrazole-7-carboxylic acid Chemical compound C12COC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1CCCC1 PHZPYPOXYQPPFG-UHFFFAOYSA-N 0.000 claims 1
- PPFCSJSDICUJFB-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3a-methyl-4,5-dihydro-3h-benzo[g]indazole-7-carboxylic acid Chemical compound CC12CCC3=CC(C(O)=O)=CC=C3C1=NN(C=1C=C(Cl)C(C#N)=CC=1)C2C1CCCC1 PPFCSJSDICUJFB-UHFFFAOYSA-N 0.000 claims 1
- PASMJJLOLQRONG-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-n-(2-hydroxyethyl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxamide Chemical compound C12CCC3=CC(C(=O)NCCO)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1CCCC1 PASMJJLOLQRONG-UHFFFAOYSA-N 0.000 claims 1
- QYFBPZRUBOWLMJ-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-n-(2-methylsulfonylethyl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxamide Chemical compound C12CCC3=CC(C(=O)NCCS(=O)(=O)C)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1CCCC1 QYFBPZRUBOWLMJ-UHFFFAOYSA-N 0.000 claims 1
- DSCXRIQRGFSVBP-UHFFFAOYSA-N 2-(3-chloro-4-cyanophenyl)-n-(2-methylsulfonylethyl)-3-(2-methyl-1,3-thiazol-5-yl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxamide Chemical compound S1C(C)=NC=C1C1N(C=2C=C(Cl)C(C#N)=CC=2)N=C2C3=CC=C(C(=O)NCCS(C)(=O)=O)C=C3CCC21 DSCXRIQRGFSVBP-UHFFFAOYSA-N 0.000 claims 1
- KNRBRFDSNFIKJR-UHFFFAOYSA-N 2-(4-cyano-3-methylphenyl)-3-(cyclopenten-1-yl)-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C1=C(C#N)C(C)=CC(N2C(C3C(C4=CC=C(C=C4CC3)C(O)=O)=N2)C=2CCCC=2)=C1 KNRBRFDSNFIKJR-UHFFFAOYSA-N 0.000 claims 1
- ISMRBSUPQBXXMD-UHFFFAOYSA-N 2-(4-cyano-3-methylphenyl)-3-(cyclopenten-1-yl)-3a,4-dihydro-3h-chromeno[4,3-c]pyrazole-7-carboxylic acid Chemical compound C1=C(C#N)C(C)=CC(N2C(C3C(C4=CC=C(C=C4OC3)C(O)=O)=N2)C=2CCCC=2)=C1 ISMRBSUPQBXXMD-UHFFFAOYSA-N 0.000 claims 1
- LBEFNCMRTYSXPH-UHFFFAOYSA-N 2-(4-cyano-3-methylphenyl)-3-cyclopentyl-3a,4-dihydro-3h-chromeno[4,3-c]pyrazole-7-carboxylic acid Chemical compound C1=C(C#N)C(C)=CC(N2C(C3C(C4=CC=C(C=C4OC3)C(O)=O)=N2)C2CCCC2)=C1 LBEFNCMRTYSXPH-UHFFFAOYSA-N 0.000 claims 1
- MHNSKVYWFDVXHV-UHFFFAOYSA-N 2-(4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C12CCC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=CC(=CC=2)C#N)C1C1CCCC1 MHNSKVYWFDVXHV-UHFFFAOYSA-N 0.000 claims 1
- IZYLHHSKJUTTDP-UHFFFAOYSA-N 2-(5-cyano-6-methylpyridin-2-yl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid Chemical compound C1=C(C#N)C(C)=NC(N2C(C3C(C4=CC=C(C=C4CC3)C(O)=O)=N2)C2CCCC2)=C1 IZYLHHSKJUTTDP-UHFFFAOYSA-N 0.000 claims 1
- ZQMUWFLXGUPXTI-UHFFFAOYSA-N 2-[4-cyano-3-(trifluoromethyl)phenyl]-3-cyclopentyl-3a,4-dihydro-3h-chromeno[4,3-c]pyrazole-7-carboxylic acid Chemical compound C12COC3=CC(C(=O)O)=CC=C3C2=NN(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1C1CCCC1 ZQMUWFLXGUPXTI-UHFFFAOYSA-N 0.000 claims 1
- FZOCKBQCTWALKE-UHFFFAOYSA-N 2-chloro-4-[3-(4-fluorophenyl)-7-hydroxy-3,3a,4,5-tetrahydrobenzo[g]indazol-2-yl]benzonitrile Chemical compound C12CCC3=CC(O)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1=CC=C(F)C=C1 FZOCKBQCTWALKE-UHFFFAOYSA-N 0.000 claims 1
- 239000005541 ACE inhibitor Substances 0.000 claims 1
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 1
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 206010048554 Endothelial dysfunction Diseases 0.000 claims 1
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims 1
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 239000002160 alpha blocker Substances 0.000 claims 1
- 229940124308 alpha-adrenoreceptor antagonist Drugs 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 108091008698 baroreceptors Proteins 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 229940030606 diuretics Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 230000008694 endothelial dysfunction Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- MZBNNMPUCTYVEZ-UHFFFAOYSA-N methyl 2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylate Chemical compound C12CCC3=CC(C(=O)OC)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1CCCC1 MZBNNMPUCTYVEZ-UHFFFAOYSA-N 0.000 claims 1
- FRSYMDSGBCVUEB-UHFFFAOYSA-N n-[2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazol-7-yl]acetamide Chemical compound C12CCC3=CC(NC(=O)C)=CC=C3C2=NN(C=2C=C(Cl)C(C#N)=CC=2)C1C1CCCC1 FRSYMDSGBCVUEB-UHFFFAOYSA-N 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 210000001774 pressoreceptor Anatomy 0.000 claims 1
- 239000002464 receptor antagonist Substances 0.000 claims 1
- 229940044551 receptor antagonist Drugs 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 229940086526 renin-inhibitors Drugs 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
-
- 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US86360606P | 2006-10-31 | 2006-10-31 | |
PCT/IB2007/003207 WO2008053300A1 (en) | 2006-10-31 | 2007-10-17 | Pyrazoline compounds as mineralocorticoid receptor antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20120078T1 true HRP20120078T1 (hr) | 2012-02-29 |
Family
ID=39027523
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20120078T HRP20120078T1 (hr) | 2006-10-31 | 2012-01-23 | Pirazolinski spojevi kao antagonisti mineralokortikoidnih receptora |
Country Status (40)
Country | Link |
---|---|
US (3) | US7781428B2 (no) |
EP (1) | EP2089367B1 (no) |
JP (1) | JP4977760B2 (no) |
KR (1) | KR101107800B1 (no) |
CN (1) | CN101541757A (no) |
AP (1) | AP2527A (no) |
AR (1) | AR063529A1 (no) |
AT (1) | ATE537151T1 (no) |
AU (1) | AU2007315884B2 (no) |
BR (1) | BRPI0717937A2 (no) |
CA (1) | CA2667966C (no) |
CL (1) | CL2007003154A1 (no) |
CO (1) | CO6160307A2 (no) |
CR (1) | CR10725A (no) |
CU (1) | CU23779B7 (no) |
CY (1) | CY1112311T1 (no) |
DK (1) | DK2089367T3 (no) |
EA (1) | EA016370B1 (no) |
ES (1) | ES2375877T3 (no) |
GE (1) | GEP20115239B (no) |
GT (1) | GT200700096A (no) |
HN (1) | HN2007000437A (no) |
HR (1) | HRP20120078T1 (no) |
IL (1) | IL198241A0 (no) |
MA (1) | MA30821B1 (no) |
MX (1) | MX2009004662A (no) |
MY (1) | MY145795A (no) |
NI (1) | NI200900071A (no) |
NO (1) | NO20091741L (no) |
NZ (1) | NZ575923A (no) |
PE (1) | PE20081472A1 (no) |
PL (1) | PL2089367T3 (no) |
PT (1) | PT2089367E (no) |
RS (2) | RS20090208A (no) |
SI (1) | SI2089367T1 (no) |
TN (1) | TN2009000160A1 (no) |
TW (1) | TWI357327B (no) |
UA (1) | UA92670C2 (no) |
UY (1) | UY30670A1 (no) |
WO (1) | WO2008053300A1 (no) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI431010B (zh) | 2007-12-19 | 2014-03-21 | Lilly Co Eli | 礦皮質素受體拮抗劑及使用方法 |
ES2759949T3 (es) * | 2009-10-29 | 2020-05-12 | Bristol Myers Squibb Co | Compuestos heterocíclicos tricíclicos |
CA2796307A1 (en) | 2010-05-10 | 2011-11-17 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and compositions for the treatment of fluid accumulation in and/ or under the retina |
JP2013528598A (ja) | 2010-05-11 | 2013-07-11 | ファイザー・インク | ミネラルコルチコイド受容体拮抗薬としてのモルホリン化合物 |
WO2011157798A1 (en) | 2010-06-16 | 2011-12-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for stimulating reepithelialisation during wound healing |
CN102372710A (zh) * | 2010-08-18 | 2012-03-14 | 山东轩竹医药科技有限公司 | 作为盐皮质激素受体拮抗剂的并环类化合物 |
US10172907B2 (en) | 2010-10-05 | 2019-01-08 | Nova Southeastern University | Compositions comprising β-arrestin 1 and methods of use thereof for therapeutic modulation of aldosterone levels in heart disease |
DK3160948T3 (en) | 2014-06-30 | 2019-02-18 | Astrazeneca Ab | BENZOXAZINONAMIDES AS MODULATORS OF MINERALOCORTICOID RECEPTORS |
JP6835836B2 (ja) | 2015-10-13 | 2021-02-24 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 脈絡膜血管新生の処置のための方法及び医薬組成物 |
EP3490606B8 (en) | 2016-07-26 | 2024-04-10 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Antagonist of mineralocorticoid receptor for the treatment of osteoarthritis |
EP3507278B1 (en) | 2016-09-02 | 2021-01-27 | Bristol-Myers Squibb Company | Substituted tricyclic heterocyclic compounds |
WO2019032632A1 (en) | 2017-08-09 | 2019-02-14 | Bristol-Myers Squibb Company | ALKYLPHENYL COMPOUNDS |
US11059784B2 (en) | 2017-08-09 | 2021-07-13 | Bristol-Myers Squibb Company | Oxime ether compounds |
CN109051490A (zh) | 2018-09-18 | 2018-12-21 | 深圳市鲸仓科技有限公司 | 可移动式密集存拣装置 |
WO2021180818A1 (en) | 2020-03-11 | 2021-09-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of determining whether a subject has or is at risk of having a central serous chorioretinopathy |
WO2023031277A1 (en) | 2021-08-31 | 2023-03-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of ocular rosacea |
CN113679716B (zh) | 2021-10-13 | 2024-03-26 | 史大永 | 溴酚-吡唑啉化合物在治疗猫冠状病毒疾病中的应用 |
CN114230457B (zh) * | 2022-01-04 | 2023-06-09 | 中山大学 | 一类2-亚苄基四氢萘酮衍生物及其制备方法和应用 |
Family Cites Families (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1086068A (en) | 1964-09-02 | 1967-10-04 | Ici Ltd | Process for the whitening of polymeric materials and nitrogen-containing polycyclic compounds for use therein |
BE789948A (fr) | 1971-10-13 | 1973-04-11 | Sandoz Sa | Nouveaux derives du pyrazole, leur preparation et leur application comme medicaments |
US3816438A (en) | 1972-12-22 | 1974-06-11 | Sandoz Ag | 2h(1)-benzothiepino(5,4-c)-pyrazoles and(1)-benzothiopyrano(4,3-c)-pyrazoles |
US3843666A (en) | 1973-05-29 | 1974-10-22 | Sandoz Ag | Process for preparing substituted indeno,naphtho and cyclohepta pyrazoles |
US4866025A (en) | 1988-09-30 | 1989-09-12 | Eastman Kodak Company | Thermally-transferable fluorescent diphenylpyrazolines |
HUT67929A (en) | 1992-01-23 | 1995-05-29 | Pfizer | Benzopyran and related ltb4 antagonists |
GB9318691D0 (en) | 1993-09-09 | 1993-10-27 | Merck Sharp & Dohme | Therapeutic agents |
AR006520A1 (es) | 1996-03-20 | 1999-09-08 | Astra Pharma Prod | Derivados de 2-arilpirazolisoquinolina y cinolinona y procedimiento para su preparacion. |
WO1998009969A1 (en) * | 1996-09-05 | 1998-03-12 | Astra Pharmaceuticals Ltd. | Novel aryl-pyridazines |
JPH10273467A (ja) | 1997-01-29 | 1998-10-13 | Snow Brand Milk Prod Co Ltd | 新規テトラロン又はベンゾピラノン誘導体及びその製造方法 |
IT1292092B1 (it) | 1997-06-05 | 1999-01-25 | Geange Ltd | Impiego di derivati eterociclici aromatici azotati nel trattamento topico di affezioni di tessuti epiteliali |
JP2002512962A (ja) | 1998-04-30 | 2002-05-08 | ビーエーエスエフ アクチェンゲゼルシャフト | プロテインキナーゼ活性を有する置換三環式ピラゾール誘導体 |
US6432974B1 (en) | 2000-02-04 | 2002-08-13 | Wyeth | Pyrrolo-isoquinoline and tetra-hydropyrrolo-isoquinoline derivatives and their use as mediators of the 5-HT7 receptor |
US7745639B2 (en) | 2002-03-08 | 2010-06-29 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
JP2006508893A (ja) | 2002-03-15 | 2006-03-16 | イーライ・リリー・アンド・カンパニー | ステロイドホルモン核内レセプターモジュレーターとしてのジヒドロインドール−2−オン誘導体 |
TW200400816A (en) | 2002-06-26 | 2004-01-16 | Lilly Co Eli | Tricyclic steroid hormone nuclear receptor modulators |
DE60308387T2 (de) | 2002-08-02 | 2007-09-20 | Vertex Pharmaceuticals Inc., Cambridge | Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren |
AU2003259475A1 (en) | 2002-09-18 | 2004-04-08 | Pfizer Products Inc. | Pyrazole derivatives as transforming growth factor (TGF) inhibitors |
CA2511806A1 (en) | 2003-01-22 | 2004-08-12 | Eli Lilly And Company | Indole-derivative modulators of steroid hormone nuclear receptors |
US7803814B2 (en) * | 2003-12-19 | 2010-09-28 | Eli Lilly And Company | Tricyclic steroid hormone nuclear receptor modulators |
JP2007230869A (ja) | 2004-04-05 | 2007-09-13 | Takeda Chem Ind Ltd | アルドステロン受容体拮抗剤 |
WO2006010142A2 (en) | 2004-07-14 | 2006-01-26 | Ligand Pharmaceuticals, Inc. | Mineralocorticoid receptor modulator compounds, processes for their preparation, and their use |
HUE041596T2 (hu) | 2004-07-30 | 2019-05-28 | Exelixis Inc | Pirrol származékok mint gyógyászati szerek |
JP5123668B2 (ja) | 2005-01-10 | 2013-01-23 | エグゼリクシス, インコーポレイテッド | 医薬品としての複素環カルボキサミド化合物 |
US20100160304A1 (en) | 2005-01-19 | 2010-06-24 | Dainippon Sumitomo Pharma Co., Ltd | Aromatic sulfone compound as aldosterone receptor modulator |
CN101115745A (zh) | 2005-02-10 | 2008-01-30 | 默克公司 | 有丝分裂驱动蛋白抑制剂 |
-
2007
- 2007-10-17 AU AU2007315884A patent/AU2007315884B2/en not_active Ceased
- 2007-10-17 JP JP2009533977A patent/JP4977760B2/ja not_active Expired - Fee Related
- 2007-10-17 PL PL07825488T patent/PL2089367T3/pl unknown
- 2007-10-17 PT PT07825488T patent/PT2089367E/pt unknown
- 2007-10-17 DK DK07825488.5T patent/DK2089367T3/da active
- 2007-10-17 EP EP07825488A patent/EP2089367B1/en active Active
- 2007-10-17 BR BRPI0717937-5A2A patent/BRPI0717937A2/pt not_active IP Right Cessation
- 2007-10-17 WO PCT/IB2007/003207 patent/WO2008053300A1/en active Application Filing
- 2007-10-17 UA UAA200903302A patent/UA92670C2/ru unknown
- 2007-10-17 AP AP2009004822A patent/AP2527A/xx active
- 2007-10-17 SI SI200730830T patent/SI2089367T1/sl unknown
- 2007-10-17 CN CNA2007800433330A patent/CN101541757A/zh active Pending
- 2007-10-17 GE GEAP200711240A patent/GEP20115239B/en unknown
- 2007-10-17 KR KR1020097008836A patent/KR101107800B1/ko not_active IP Right Cessation
- 2007-10-17 MY MYPI20091613A patent/MY145795A/en unknown
- 2007-10-17 MX MX2009004662A patent/MX2009004662A/es active IP Right Grant
- 2007-10-17 AT AT07825488T patent/ATE537151T1/de active
- 2007-10-17 RS RSP-2009/0208A patent/RS20090208A/sr unknown
- 2007-10-17 ES ES07825488T patent/ES2375877T3/es active Active
- 2007-10-17 RS RS20120051A patent/RS52203B/en unknown
- 2007-10-17 EA EA200970341A patent/EA016370B1/ru not_active IP Right Cessation
- 2007-10-17 CA CA2667966A patent/CA2667966C/en not_active Expired - Fee Related
- 2007-10-17 NZ NZ575923A patent/NZ575923A/en not_active IP Right Cessation
- 2007-10-24 US US11/923,248 patent/US7781428B2/en not_active Expired - Fee Related
- 2007-10-29 AR ARP070104787A patent/AR063529A1/es not_active Application Discontinuation
- 2007-10-29 UY UY30670A patent/UY30670A1/es not_active Application Discontinuation
- 2007-10-30 TW TW096140838A patent/TWI357327B/zh not_active IP Right Cessation
- 2007-10-30 GT GT200700096A patent/GT200700096A/es unknown
- 2007-10-30 PE PE2007001482A patent/PE20081472A1/es not_active Application Discontinuation
- 2007-10-31 CL CL200703154A patent/CL2007003154A1/es unknown
- 2007-10-31 HN HN2007000437A patent/HN2007000437A/es unknown
-
2009
- 2009-04-17 CU CU20090058A patent/CU23779B7/es not_active IP Right Cessation
- 2009-04-17 CR CR10725A patent/CR10725A/es not_active Application Discontinuation
- 2009-04-20 IL IL198241A patent/IL198241A0/en unknown
- 2009-04-21 CO CO09040130A patent/CO6160307A2/es unknown
- 2009-04-24 TN TNP2009000160A patent/TN2009000160A1/fr unknown
- 2009-04-29 NI NI200900071A patent/NI200900071A/es unknown
- 2009-04-30 MA MA31831A patent/MA30821B1/fr unknown
- 2009-05-04 NO NO20091741A patent/NO20091741L/no not_active Application Discontinuation
-
2010
- 2010-07-12 US US12/834,117 patent/US20100280016A1/en not_active Abandoned
-
2011
- 2011-10-20 US US13/277,270 patent/US20120035131A1/en not_active Abandoned
-
2012
- 2012-01-23 CY CY20121100076T patent/CY1112311T1/el unknown
- 2012-01-23 HR HR20120078T patent/HRP20120078T1/hr unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20120078T1 (hr) | Pirazolinski spojevi kao antagonisti mineralokortikoidnih receptora | |
CA2401502A1 (en) | Carboxylic acid derivatives as ip antagonists | |
RU2013114771A (ru) | Диамиды азетидинила как ингибиторы моноацилглицерол липазы | |
HRP20100633T1 (hr) | Derivati piridazinona kao agonisti receptora tiroidnih hormona | |
MA37866B1 (fr) | Dérivés de type aza-indazole ou diaza-indazole pour le traitement de la douleur | |
PE20081228A1 (es) | Compuesto heteromonociclico | |
EA022420B1 (ru) | Гетероциклические ингибиторы глутаминилциклазы (qc, ec 2.3.2.5) | |
EA201000024A1 (ru) | Новые производные дикарбоновых кислот в качестве агонистов рецептора s1p1 | |
HRP20130976T1 (hr) | Karbonilaminopirolopirazoli, potentni inhibitori kinaza | |
HRP20140919T1 (hr) | Spojevi koji moduliraju androgene receptore | |
ATE540932T1 (de) | Hydantoin-derivate als antibakterielle wirkstoffe | |
HRP20130738T1 (hr) | Postupak lijeäśenja ili profilakse | |
PE20110226A1 (es) | Daa-piridina como ligando del receptor periferico de benzodiazepina | |
AP2001002307A0 (en) | B3 adrenergic receptor agonists and uses thereof. | |
HRP20150049T1 (hr) | Derivati oksazolil-metiletera kao agonisti alx-receptora | |
MA31684B1 (fr) | Composition pharmaceutique contenant un antagoniste des canaux calciques de type dihydropyridine et son procédé de préparation | |
MXPA04004312A (es) | Combinacion de inhibidor de ciclooxigenasa-2/inhibidor de desacetilasa de histona. | |
HRP20231608T1 (hr) | Derivati piridinil sulfonamida, njihovi farmaceutski pripravci i njihove uporabe | |
MX2012001160A (es) | Agonistas del receptor de esfingosina-1-fosfato. | |
EA200970793A1 (ru) | Модуляторы рецепторов, активируемых пролифераторами пероксисом | |
MA30704B1 (fr) | Compositions therapeutiques | |
TW200716597A (en) | Novel piperidine-substituted indoles | |
HRP20120231T1 (hr) | Upotreba derivata indola kao aktivatora nurr-1 u liječenju parkinsonove bolesti | |
NZ600266A (en) | Compound, certain novel forms thereof, pharmaceutical compositions thereof and methods for preparation and use | |
WO2008127300A3 (en) | Oxazolidinone derivatives and methods of use |