MXPA02009071A - Compuestos con actividad agonista de 5-ht 1a para tratar glaucoma.. - Google Patents
Compuestos con actividad agonista de 5-ht 1a para tratar glaucoma..Info
- Publication number
- MXPA02009071A MXPA02009071A MXPA02009071A MXPA02009071A MXPA02009071A MX PA02009071 A MXPA02009071 A MX PA02009071A MX PA02009071 A MXPA02009071 A MX PA02009071A MX PA02009071 A MXPA02009071 A MX PA02009071A MX PA02009071 A MXPA02009071 A MX PA02009071A
- Authority
- MX
- Mexico
- Prior art keywords
- compound
- compounds
- aminopropyl
- iop
- group
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract description 59
- 230000000694 effects Effects 0.000 claims abstract description 14
- 206010061323 Optic neuropathy Diseases 0.000 claims abstract description 9
- 208000020911 optic nerve disease Diseases 0.000 claims abstract description 9
- 239000000556 agonist Substances 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 17
- 108020003175 receptors Proteins 0.000 claims description 12
- 102000005962 receptors Human genes 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 9
- 230000003247 decreasing effect Effects 0.000 claims description 9
- -1 unoproston Chemical compound 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 8
- 230000000324 neuroprotective effect Effects 0.000 claims description 8
- 102000056834 5-HT2 Serotonin Receptors Human genes 0.000 claims description 7
- 108091005479 5-HT2 receptors Proteins 0.000 claims description 7
- LYPCGXKCQDYTFV-UHFFFAOYSA-N alpha-methylserotonin Chemical compound C1=C(O)C=C2C(CC(N)C)=CNC2=C1 LYPCGXKCQDYTFV-UHFFFAOYSA-N 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 239000005557 antagonist Substances 0.000 claims description 5
- 230000007423 decrease Effects 0.000 claims description 5
- 239000003446 ligand Substances 0.000 claims description 5
- 208000001953 Hypotension Diseases 0.000 claims description 3
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 claims description 3
- 239000002876 beta blocker Substances 0.000 claims description 3
- 229940097320 beta blocking agent Drugs 0.000 claims description 3
- AQOKCDNYWBIDND-FTOWTWDKSA-N bimatoprost Chemical compound CCNC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)CCC1=CC=CC=C1 AQOKCDNYWBIDND-FTOWTWDKSA-N 0.000 claims description 3
- 229960002470 bimatoprost Drugs 0.000 claims description 3
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 claims description 3
- 208000021822 hypotensive Diseases 0.000 claims description 3
- 230000001077 hypotensive effect Effects 0.000 claims description 3
- 229960001160 latanoprost Drugs 0.000 claims description 3
- GGXICVAJURFBLW-CEYXHVGTSA-N latanoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1 GGXICVAJURFBLW-CEYXHVGTSA-N 0.000 claims description 3
- 150000002632 lipids Chemical class 0.000 claims description 3
- 230000003547 miosis Effects 0.000 claims description 3
- 239000003604 miotic agent Substances 0.000 claims description 3
- 229960002368 travoprost Drugs 0.000 claims description 3
- MKPLKVHSHYCHOC-AHTXBMBWSA-N travoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC=CC(C(F)(F)F)=C1 MKPLKVHSHYCHOC-AHTXBMBWSA-N 0.000 claims description 3
- 150000003180 prostaglandins Chemical class 0.000 claims 3
- IZYIHUIJXWQHNH-UHFFFAOYSA-N 1-(2-aminopropyl)indol-6-ol Chemical compound C1=C(O)C=C2N(CC(N)C)C=CC2=C1 IZYIHUIJXWQHNH-UHFFFAOYSA-N 0.000 claims 2
- XXCLNSYNUQMDML-UHFFFAOYSA-N 1-(5-chloroindol-1-yl)propan-2-amine Chemical compound ClC1=CC=C2N(CC(N)C)C=CC2=C1 XXCLNSYNUQMDML-UHFFFAOYSA-N 0.000 claims 2
- VUGMRGBLFJISLF-UHFFFAOYSA-N 1-(6-methoxyindol-1-yl)propan-2-amine Chemical compound COC1=CC=C2C=CN(CC(C)N)C2=C1 VUGMRGBLFJISLF-UHFFFAOYSA-N 0.000 claims 2
- JTEJPPKMYBDEMY-UHFFFAOYSA-N 5-Methoxytryptamine Natural products COC1=CC=C2NC=C(CCN)C2=C1 JTEJPPKMYBDEMY-UHFFFAOYSA-N 0.000 claims 2
- 229940097276 5-methoxytryptamine Drugs 0.000 claims 2
- 125000003259 prostaglandin group Chemical class 0.000 claims 2
- 239000003723 serotonin 1A agonist Substances 0.000 abstract description 3
- 239000002399 serotonin 2A agonist Substances 0.000 abstract description 2
- 230000004410 intraocular pressure Effects 0.000 description 26
- 238000012360 testing method Methods 0.000 description 17
- 238000000034 method Methods 0.000 description 16
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 16
- 208000010412 Glaucoma Diseases 0.000 description 14
- 241000700159 Rattus Species 0.000 description 13
- 210000004027 cell Anatomy 0.000 description 13
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 10
- 238000009472 formulation Methods 0.000 description 10
- 239000003981 vehicle Substances 0.000 description 9
- 239000012528 membrane Substances 0.000 description 8
- 230000000699 topical effect Effects 0.000 description 8
- 239000011780 sodium chloride Substances 0.000 description 7
- 229940079593 drug Drugs 0.000 description 6
- 238000011534 incubation Methods 0.000 description 6
- 230000003389 potentiating effect Effects 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- 229940054534 ophthalmic solution Drugs 0.000 description 5
- BXGJHWHRRBSQBO-WLHGVMLRSA-N (e)-but-2-enedioic acid;1-(6-methoxyindol-1-yl)propan-2-amine Chemical compound OC(=O)\C=C\C(O)=O.COC1=CC=C2C=CN(CC(C)N)C2=C1 BXGJHWHRRBSQBO-WLHGVMLRSA-N 0.000 description 4
- OHCQJHSOBUTRHG-KGGHGJDLSA-N FORSKOLIN Chemical compound O=C([C@@]12O)C[C@](C)(C=C)O[C@]1(C)[C@@H](OC(=O)C)[C@@H](O)[C@@H]1[C@]2(C)[C@@H](O)CCC1(C)C OHCQJHSOBUTRHG-KGGHGJDLSA-N 0.000 description 4
- 206010030348 Open-Angle Glaucoma Diseases 0.000 description 4
- 230000001276 controlling effect Effects 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 229960000367 inositol Drugs 0.000 description 4
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 210000001525 retina Anatomy 0.000 description 4
- 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 3
- ASXGJMSKWNBENU-UHFFFAOYSA-N 8-OH-DPAT Chemical compound C1=CC(O)=C2CC(N(CCC)CCC)CCC2=C1 ASXGJMSKWNBENU-UHFFFAOYSA-N 0.000 description 3
- XYLJNLCSTIOKRM-UHFFFAOYSA-N Alphagan Chemical compound C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 XYLJNLCSTIOKRM-UHFFFAOYSA-N 0.000 description 3
- 241000282693 Cercopithecidae Species 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- 241000283973 Oryctolagus cuniculus Species 0.000 description 3
- 208000017442 Retinal disease Diseases 0.000 description 3
- 206010038923 Retinopathy Diseases 0.000 description 3
- 229960004324 betaxolol Drugs 0.000 description 3
- NWIUTZDMDHAVTP-UHFFFAOYSA-N betaxolol Chemical compound C1=CC(OCC(O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-UHFFFAOYSA-N 0.000 description 3
- 210000004556 brain Anatomy 0.000 description 3
- 229960003679 brimonidine Drugs 0.000 description 3
- 210000003128 head Anatomy 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 239000002609 medium Substances 0.000 description 3
- 230000004112 neuroprotection Effects 0.000 description 3
- 239000002997 ophthalmic solution Substances 0.000 description 3
- 210000001328 optic nerve Anatomy 0.000 description 3
- 239000006174 pH buffer Substances 0.000 description 3
- 150000003906 phosphoinositides Chemical class 0.000 description 3
- 239000003755 preservative agent Substances 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 108090000623 proteins and genes Proteins 0.000 description 3
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 3
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 2
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 2
- XKRFYHLGVUSROY-UHFFFAOYSA-N Argon Chemical compound [Ar] XKRFYHLGVUSROY-UHFFFAOYSA-N 0.000 description 2
- 241000699802 Cricetulus griseus Species 0.000 description 2
- SUZLHDUTVMZSEV-UHFFFAOYSA-N Deoxycoleonol Natural products C12C(=O)CC(C)(C=C)OC2(C)C(OC(=O)C)C(O)C2C1(C)C(O)CCC2(C)C SUZLHDUTVMZSEV-UHFFFAOYSA-N 0.000 description 2
- 102100024785 Fibroblast growth factor 2 Human genes 0.000 description 2
- 108090000379 Fibroblast growth factor 2 Proteins 0.000 description 2
- 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 2
- 206010020772 Hypertension Diseases 0.000 description 2
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 2
- DRBBFCLWYRJSJZ-UHFFFAOYSA-N N-phosphocreatine Chemical compound OC(=O)CN(C)C(=N)NP(O)(O)=O DRBBFCLWYRJSJZ-UHFFFAOYSA-N 0.000 description 2
- 229910019142 PO4 Inorganic materials 0.000 description 2
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 2
- 229920002873 Polyethylenimine Polymers 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- VZTDIZULWFCMLS-UHFFFAOYSA-N ammonium formate Chemical compound [NH4+].[O-]C=O VZTDIZULWFCMLS-UHFFFAOYSA-N 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 238000013375 chromatographic separation Methods 0.000 description 2
- OHCQJHSOBUTRHG-UHFFFAOYSA-N colforsin Natural products OC12C(=O)CC(C)(C=C)OC1(C)C(OC(=O)C)C(O)C1C2(C)C(O)CCC1(C)C OHCQJHSOBUTRHG-UHFFFAOYSA-N 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 238000001914 filtration Methods 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 235000019253 formic acid Nutrition 0.000 description 2
- 230000005714 functional activity Effects 0.000 description 2
- 238000011990 functional testing Methods 0.000 description 2
- 239000003365 glass fiber Substances 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 230000000971 hippocampal effect Effects 0.000 description 2
- 230000001631 hypertensive effect Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- KWGKDLIKAYFUFQ-UHFFFAOYSA-M lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 description 2
- 229940100654 ophthalmic suspension Drugs 0.000 description 2
- 239000004031 partial agonist Substances 0.000 description 2
- 239000008188 pellet Substances 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- 235000021317 phosphate Nutrition 0.000 description 2
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 description 2
- 230000004224 protection Effects 0.000 description 2
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 2
- 230000000862 serotonergic effect Effects 0.000 description 2
- 229940076279 serotonin Drugs 0.000 description 2
- 239000003478 serotonin 5-HT2 receptor agonist Substances 0.000 description 2
- 238000004611 spectroscopical analysis Methods 0.000 description 2
- 238000013222 sprague-dawley male rat Methods 0.000 description 2
- 238000010254 subcutaneous injection Methods 0.000 description 2
- 239000007929 subcutaneous injection Substances 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 239000006228 supernatant Substances 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 238000003828 vacuum filtration Methods 0.000 description 2
- QCHFTSOMWOSFHM-WPRPVWTQSA-N (+)-Pilocarpine Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 description 1
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 description 1
- 229930182837 (R)-adrenaline Natural products 0.000 description 1
- GGUSQTSTQSHJAH-FQEVSTJZSA-N (R)-eliprodil Chemical compound C([C@H](O)C=1C=CC(Cl)=CC=1)N(CC1)CCC1CC1=CC=C(F)C=C1 GGUSQTSTQSHJAH-FQEVSTJZSA-N 0.000 description 1
- NWIUTZDMDHAVTP-KRWDZBQOSA-N (S)-betaxolol Chemical compound C1=CC(OC[C@@H](O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-KRWDZBQOSA-N 0.000 description 1
- TWBNMYSKRDRHAT-RCWTXCDDSA-N (S)-timolol hemihydrate Chemical compound O.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1 TWBNMYSKRDRHAT-RCWTXCDDSA-N 0.000 description 1
- TUZFHNWMUXXNGF-WLHGVMLRSA-N (e)-but-2-enedioic acid;1-(5-chloroindol-1-yl)propan-2-amine Chemical compound OC(=O)\C=C\C(O)=O.ClC1=CC=C2N(CC(N)C)C=CC2=C1 TUZFHNWMUXXNGF-WLHGVMLRSA-N 0.000 description 1
- PCJYNNYRYHEUNO-WLHGVMLRSA-N 1-(2-aminopropyl)indol-6-ol;(e)-but-2-enedioic acid Chemical compound OC(=O)\C=C\C(O)=O.C1=C(O)C=C2N(CC(N)C)C=CC2=C1 PCJYNNYRYHEUNO-WLHGVMLRSA-N 0.000 description 1
- GGUSQTSTQSHJAH-UHFFFAOYSA-N 1-(4-chlorophenyl)-2-[4-(4-fluorobenzyl)piperidin-1-yl]ethanol Chemical compound C=1C=C(Cl)C=CC=1C(O)CN(CC1)CCC1CC1=CC=C(F)C=C1 GGUSQTSTQSHJAH-UHFFFAOYSA-N 0.000 description 1
- AGJBKFAPBKOEGA-UHFFFAOYSA-M 2-methoxyethylmercury(1+);acetate Chemical compound COCC[Hg]OC(C)=O AGJBKFAPBKOEGA-UHFFFAOYSA-M 0.000 description 1
- APIXJSLKIYYUKG-UHFFFAOYSA-N 3 Isobutyl 1 methylxanthine Chemical compound O=C1N(C)C(=O)N(CC(C)C)C2=C1N=CN2 APIXJSLKIYYUKG-UHFFFAOYSA-N 0.000 description 1
- ARIRHJYRGNURLG-UHFFFAOYSA-N 3-(2-aminopropyl)-1H-indol-5-ol Chemical compound C1=C(O)C=C2C(CC(N)C)=CNC2=C1.C1=C(O)C=C2C(CC(N)C)=CNC2=C1 ARIRHJYRGNURLG-UHFFFAOYSA-N 0.000 description 1
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- HIHZDNKKIUQQSC-UHFFFAOYSA-N 6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propylamino]-1,3,5-trimethylpyrimidine-2,4-dione Chemical compound COC1=CC=CC=C1N1CCN(CCCNC=2N(C(=O)N(C)C(=O)C=2C)C)CC1 HIHZDNKKIUQQSC-UHFFFAOYSA-N 0.000 description 1
- CPXKXLSFUJLYFN-UHFFFAOYSA-N 8-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol Chemical compound C1=CC(O)=C2C(N(CCC)CCC)CCCC2=C1 CPXKXLSFUJLYFN-UHFFFAOYSA-N 0.000 description 1
- GJCOSYZMQJWQCA-UHFFFAOYSA-N 9H-xanthene Chemical compound C1=CC=C2CC3=CC=CC=C3OC2=C1 GJCOSYZMQJWQCA-UHFFFAOYSA-N 0.000 description 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 201000002862 Angle-Closure Glaucoma Diseases 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 108090000715 Brain-derived neurotrophic factor Proteins 0.000 description 1
- 102000004219 Brain-derived neurotrophic factor Human genes 0.000 description 1
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 1
- 108010005939 Ciliary Neurotrophic Factor Proteins 0.000 description 1
- 102100031614 Ciliary neurotrophic factor Human genes 0.000 description 1
- 102000004420 Creatine Kinase Human genes 0.000 description 1
- 108010042126 Creatine kinase Proteins 0.000 description 1
- IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-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
- 208000003098 Ganglion Cysts Diseases 0.000 description 1
- CEAZRRDELHUEMR-URQXQFDESA-N Gentamicin Chemical compound O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N CEAZRRDELHUEMR-URQXQFDESA-N 0.000 description 1
- 229930182566 Gentamicin Natural products 0.000 description 1
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- OMCPLEZZPVJJIS-UHFFFAOYSA-N Hypadil (TN) Chemical compound C1C(O[N+]([O-])=O)COC2=C1C=CC=C2OCC(O)CNC(C)C OMCPLEZZPVJJIS-UHFFFAOYSA-N 0.000 description 1
- YQEZLKZALYSWHR-UHFFFAOYSA-N Ketamine Chemical compound C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 241000282567 Macaca fascicularis Species 0.000 description 1
- RLJFTICUTYVZDG-UHFFFAOYSA-N Methiothepine Chemical compound C12=CC(SC)=CC=C2SC2=CC=CC=C2CC1N1CCN(C)CC1 RLJFTICUTYVZDG-UHFFFAOYSA-N 0.000 description 1
- 206010067013 Normal tension glaucoma Diseases 0.000 description 1
- 239000004743 Polypropylene Substances 0.000 description 1
- KCLANYCVBBTKTO-UHFFFAOYSA-N Proparacaine Chemical compound CCCOC1=CC=C(C(=O)OCCN(CC)CC)C=C1N KCLANYCVBBTKTO-UHFFFAOYSA-N 0.000 description 1
- QCHFTSOMWOSFHM-UHFFFAOYSA-N SJ000285536 Natural products C1OC(=O)C(CC)C1CC1=CN=CN1C QCHFTSOMWOSFHM-UHFFFAOYSA-N 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 208000005400 Synovial Cyst Diseases 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- 102000014384 Type C Phospholipases Human genes 0.000 description 1
- 108010079194 Type C Phospholipases Proteins 0.000 description 1
- IVOMOUWHDPKRLL-UHFFFAOYSA-N UNPD107823 Natural products O1C2COP(O)(=O)OC2C(O)C1N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-UHFFFAOYSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 102000030621 adenylate cyclase Human genes 0.000 description 1
- 108060000200 adenylate cyclase Proteins 0.000 description 1
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 230000002460 anti-migrenic effect Effects 0.000 description 1
- 229940006138 antiglaucoma drug and miotics prostaglandin analogues Drugs 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 229910052786 argon Inorganic materials 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- 229960000722 brinzolamide Drugs 0.000 description 1
- HCRKCZRJWPKOAR-JTQLQIEISA-N brinzolamide Chemical compound CCN[C@H]1CN(CCCOC)S(=O)(=O)C2=C1C=C(S(N)(=O)=O)S2 HCRKCZRJWPKOAR-JTQLQIEISA-N 0.000 description 1
- 239000007975 buffered saline Substances 0.000 description 1
- 239000001110 calcium chloride Substances 0.000 description 1
- 235000011148 calcium chloride Nutrition 0.000 description 1
- 229910001628 calcium chloride Inorganic materials 0.000 description 1
- 230000008061 calcium-channel-blocking effect Effects 0.000 description 1
- 244000309466 calf Species 0.000 description 1
- 229960001222 carteolol Drugs 0.000 description 1
- LWAFSWPYPHEXKX-UHFFFAOYSA-N carteolol Chemical compound N1C(=O)CCC2=C1C=CC=C2OCC(O)CNC(C)(C)C LWAFSWPYPHEXKX-UHFFFAOYSA-N 0.000 description 1
- 210000003710 cerebral cortex Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229940125904 compound 1 Drugs 0.000 description 1
- 229940125782 compound 2 Drugs 0.000 description 1
- 229940126214 compound 3 Drugs 0.000 description 1
- 229940125898 compound 5 Drugs 0.000 description 1
- 238000004590 computer program Methods 0.000 description 1
- 238000011461 current therapy Methods 0.000 description 1
- 229940095074 cyclic amp Drugs 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000006185 dispersion Substances 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
- 229960003933 dorzolamide Drugs 0.000 description 1
- IAVUPMFITXYVAF-XPUUQOCRSA-N dorzolamide Chemical compound CCN[C@H]1C[C@H](C)S(=O)(=O)C2=C1C=C(S(N)(=O)=O)S2 IAVUPMFITXYVAF-XPUUQOCRSA-N 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 238000002571 electroretinography Methods 0.000 description 1
- 230000004406 elevated intraocular pressure Effects 0.000 description 1
- 229950005455 eliprodil Drugs 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 229960005139 epinephrine Drugs 0.000 description 1
- DEFVIWRASFVYLL-UHFFFAOYSA-N ethylene glycol bis(2-aminoethyl)tetraacetic acid Chemical compound OC(=O)CN(CC(O)=O)CCOCCOCCN(CC(O)=O)CC(O)=O DEFVIWRASFVYLL-UHFFFAOYSA-N 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 239000003885 eye ointment Substances 0.000 description 1
- 230000001605 fetal effect Effects 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 229960002518 gentamicin Drugs 0.000 description 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000000265 homogenisation Methods 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 1
- 229960003299 ketamine Drugs 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 229960004771 levobetaxolol Drugs 0.000 description 1
- 229960000831 levobunolol Drugs 0.000 description 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 description 1
- 238000000670 ligand binding assay Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 201000002978 low tension glaucoma Diseases 0.000 description 1
- UEGPKNKPLBYCNK-UHFFFAOYSA-L magnesium acetate Chemical compound [Mg+2].CC([O-])=O.CC([O-])=O UEGPKNKPLBYCNK-UHFFFAOYSA-L 0.000 description 1
- 239000011654 magnesium acetate Substances 0.000 description 1
- 235000011285 magnesium acetate Nutrition 0.000 description 1
- 229940069446 magnesium acetate Drugs 0.000 description 1
- 229910052943 magnesium sulfate Inorganic materials 0.000 description 1
- 235000019341 magnesium sulphate Nutrition 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 229960005254 naratriptan Drugs 0.000 description 1
- UNHGSHHVDNGCFN-UHFFFAOYSA-N naratriptan Chemical compound C=12[CH]C(CCS(=O)(=O)NC)=CC=C2N=CC=1C1CCN(C)CC1 UNHGSHHVDNGCFN-UHFFFAOYSA-N 0.000 description 1
- 210000004126 nerve fiber Anatomy 0.000 description 1
- 229950000754 nipradilol Drugs 0.000 description 1
- 229940100655 ophthalmic gel Drugs 0.000 description 1
- 229940069265 ophthalmic ointment Drugs 0.000 description 1
- 210000003733 optic disk Anatomy 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
- 238000007539 photo-oxidation reaction Methods 0.000 description 1
- 108091008695 photoreceptors Proteins 0.000 description 1
- 229960001416 pilocarpine Drugs 0.000 description 1
- 229920001467 poly(styrenesulfonates) Polymers 0.000 description 1
- 239000004417 polycarbonate Substances 0.000 description 1
- 229920000515 polycarbonate Polymers 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 229960003981 proparacaine Drugs 0.000 description 1
- 229960003712 propranolol Drugs 0.000 description 1
- 239000002287 radioligand Substances 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000002207 retinal effect Effects 0.000 description 1
- 210000003583 retinal pigment epithelium Anatomy 0.000 description 1
- 238000003345 scintillation counting Methods 0.000 description 1
- 239000000952 serotonin receptor agonist Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000012679 serum free medium Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229960003708 sumatriptan Drugs 0.000 description 1
- KQKPFRSPSRPDEB-UHFFFAOYSA-N sumatriptan Chemical compound CNS(=O)(=O)CC1=CC=C2NC=C(CCN(C)C)C2=C1 KQKPFRSPSRPDEB-UHFFFAOYSA-N 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000001839 systemic circulation Effects 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229960004605 timolol Drugs 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 239000012929 tonicity agent Substances 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 238000012876 topography Methods 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 description 1
- 229960001600 xylazine Drugs 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
- A61K31/495—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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
- A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Ophthalmology & Optometry (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (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)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Crystals, And After-Treatments Of Crystals (AREA)
- Liquid Crystal Substances (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19027900P | 2000-03-17 | 2000-03-17 | |
| PCT/US2001/005432 WO2001070223A1 (en) | 2000-03-17 | 2001-02-20 | Compounds with 5-ht2 and 5-ht1a agonist activity for treating glaucoma |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA02009071A true MXPA02009071A (es) | 2003-05-23 |
Family
ID=22700682
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA02009071A MXPA02009071A (es) | 2000-03-17 | 2001-02-20 | Compuestos con actividad agonista de 5-ht 1a para tratar glaucoma.. |
| MXPA02009072A MXPA02009072A (es) | 2000-03-17 | 2001-02-23 | Compuestos con actividad de 5-ht1a utiles para tratar trastornos de la retina exterior. |
| MXPA02009073A MXPA02009073A (es) | 2000-03-17 | 2001-02-23 | Compuestos con actividad de 5-ht1a utiles para controlar la perdida del campo visual. |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA02009072A MXPA02009072A (es) | 2000-03-17 | 2001-02-23 | Compuestos con actividad de 5-ht1a utiles para tratar trastornos de la retina exterior. |
| MXPA02009073A MXPA02009073A (es) | 2000-03-17 | 2001-02-23 | Compuestos con actividad de 5-ht1a utiles para controlar la perdida del campo visual. |
Country Status (18)
| Country | Link |
|---|---|
| EP (3) | EP1263434A1 (OSRAM) |
| JP (5) | JP2003527423A (OSRAM) |
| KR (3) | KR20030016239A (OSRAM) |
| CN (2) | CN1418100A (OSRAM) |
| AR (1) | AR028258A1 (OSRAM) |
| AT (1) | ATE247507T1 (OSRAM) |
| AU (5) | AU2001238552A1 (OSRAM) |
| BR (3) | BR0109193A (OSRAM) |
| CA (3) | CA2400637A1 (OSRAM) |
| DE (1) | DE60100625T2 (OSRAM) |
| DK (1) | DK1263504T3 (OSRAM) |
| ES (1) | ES2204848T3 (OSRAM) |
| MX (3) | MXPA02009071A (OSRAM) |
| PL (1) | PL203709B1 (OSRAM) |
| PT (1) | PT1263504E (OSRAM) |
| TW (1) | TWI268777B (OSRAM) |
| WO (3) | WO2001070223A1 (OSRAM) |
| ZA (1) | ZA200206350B (OSRAM) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6960579B1 (en) | 1998-05-19 | 2005-11-01 | Alcon Manufacturing, Ltd. | Serotonergic 5HT7 receptor compounds for treating ocular and CNS disorders |
| EP1263434A1 (en) * | 2000-03-17 | 2002-12-11 | Alcon, Inc | Compounds with 5-ht 2 and 5-ht 1a agonist activity for treating glaucoma |
| US20030207890A1 (en) | 2001-02-23 | 2003-11-06 | Collier Robert J | Compounds with 5-ht1a activity useful for treating disorders of the outer retina |
| TW593302B (en) * | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
| EP1581209A4 (en) | 2002-12-13 | 2009-03-11 | Alcon Inc | NEW BENZOPYRAN ANALOGUE AND ITS USE FOR THE TREATMENT OF GLAUKOM |
| JP2004262812A (ja) * | 2003-02-28 | 2004-09-24 | Rohto Pharmaceut Co Ltd | 眼圧低下剤 |
| EP1617838A4 (en) * | 2003-04-25 | 2011-07-06 | Mitsubishi Tanabe Pharma Corp | COMPOSITION FOR ORAL ADMINISTRATION WITH ALKYLENEDIOXYBENZOLE DERIVATIVES |
| WO2005053688A1 (en) | 2003-11-26 | 2005-06-16 | Alcon, Inc. | Substituted furo[2,3-g] indazoles for the treatment of glaucoma |
| US7338972B1 (en) | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
| WO2005058911A2 (en) | 2003-12-15 | 2005-06-30 | Alcon, Inc. | Substituted [1,4]oxazino[2,3-g]indazoles for the treatment of glaucoma |
| US7129257B1 (en) | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
| US20050244463A1 (en) | 2004-04-30 | 2005-11-03 | Allergan, Inc. | Sustained release intraocular implants and methods for treating ocular vasculopathies |
| EP2248524A3 (en) | 2004-08-25 | 2011-03-09 | Takeda Pharmaceutical Company Limited | Preventives/remedies for stress urinary incontinence and method of screening the same |
| US7425572B2 (en) | 2004-12-08 | 2008-09-16 | Alcon, Inc. | Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma |
| WO2007132841A1 (ja) | 2006-05-16 | 2007-11-22 | Takeda Pharmaceutical Company Limited | 縮合複素環化合物およびその用途 |
| WO2008024846A2 (en) * | 2006-08-25 | 2008-02-28 | Allergan, Inc. | Brimonidine and timolol compositions |
| EP2896624B1 (en) | 2007-03-28 | 2016-07-13 | Atir Holding S.A. | Heterotricyclic compounds as serotonergic and/or dopaminergic agents and uses thereof |
| JP5520051B2 (ja) | 2007-11-15 | 2014-06-11 | 武田薬品工業株式会社 | 縮合ピリジン誘導体およびその用途 |
| TW201010727A (en) * | 2008-09-03 | 2010-03-16 | Alcon Res Ltd | Pharmaceutical composition having relatively low ionic strength |
| DK2498783T3 (en) | 2009-11-09 | 2018-12-10 | Allergan Inc | COMPOSITIONS AND PROCEDURES FOR STIMULATING HAIR GROWTH |
| WO2011071136A1 (ja) | 2009-12-11 | 2011-06-16 | アステラス製薬株式会社 | 線維筋痛症治療剤 |
| RU2641021C2 (ru) | 2013-02-15 | 2018-01-17 | Аллерган, Инк. | Имплантат для пролонгированной доставки лекарственного средства |
| WO2018064465A1 (en) | 2016-09-29 | 2018-04-05 | The Regents Of The University Of California | Compounds for increasing neural plasticity |
| WO2019131902A1 (ja) | 2017-12-27 | 2019-07-04 | 武田薬品工業株式会社 | 腹圧性尿失禁および便失禁の治療薬 |
| BR112021016620A2 (pt) | 2019-02-27 | 2021-11-03 | Univ California | Azepino-indóis e outros heterociclos para o tratamento de distúrbios cerebrais |
| JP7636796B2 (ja) | 2019-02-27 | 2025-02-27 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 脳障害を治療するためのｎ－置換インドール及び他の複素環化合物 |
| CA3239565A1 (en) | 2021-12-15 | 2023-06-22 | Delix Therapeutics, Inc. | Phenoxy and benzyloxy substituted psychoplastogens and uses thereof |
| IL313499A (en) * | 2021-12-23 | 2024-08-01 | Cilcare Dev | Derivatives of 4-phenyl-tetrahydropyridine for the treatment of hearing diseases |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH02262518A (ja) * | 1989-04-03 | 1990-10-25 | Kaken Pharmaceut Co Ltd | 眼圧調整剤 |
| JP2824863B2 (ja) * | 1989-07-12 | 1998-11-18 | エーザイ株式会社 | α▲下１▼―ブロッカー点眼剤 |
| TW270114B (OSRAM) * | 1993-10-22 | 1996-02-11 | Hoffmann La Roche | |
| US5521183A (en) * | 1994-08-30 | 1996-05-28 | Allergan | Use of 5-HT ligands as anti-pruritic agents |
| JP3958391B2 (ja) * | 1995-10-25 | 2007-08-15 | 三菱化学株式会社 | 眼疾患用薬剤 |
| US5998467A (en) * | 1995-10-25 | 1999-12-07 | Mitsubishi Chemical Corporation | Medicine for oculopathy |
| WO1998018458A1 (en) * | 1996-10-31 | 1998-05-07 | Alcon Laboratories, Inc. | Opthalmological compositions containing serotonin 5-ht1a receptor agonist and their use in the treatment of glaucoma |
| DE19751949A1 (de) * | 1997-11-24 | 1999-05-27 | Bayer Ag | Verwendung von substituierten Aminomethyl-Chromanen zur Verhinderung der neuronalen Degeneration und zur Förderung der neuronalen Regeneration |
| GB9819033D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds VI |
| EP1263434A1 (en) * | 2000-03-17 | 2002-12-11 | Alcon, Inc | Compounds with 5-ht 2 and 5-ht 1a agonist activity for treating glaucoma |
-
2001
- 2001-02-20 EP EP01911005A patent/EP1263434A1/en not_active Withdrawn
- 2001-02-20 MX MXPA02009071A patent/MXPA02009071A/es unknown
- 2001-02-20 BR BR0109193-0A patent/BR0109193A/pt not_active Application Discontinuation
- 2001-02-20 WO PCT/US2001/005432 patent/WO2001070223A1/en not_active Ceased
- 2001-02-20 KR KR1020027012169A patent/KR20030016239A/ko not_active Withdrawn
- 2001-02-20 AU AU2001238552A patent/AU2001238552A1/en not_active Abandoned
- 2001-02-20 JP JP2001568421A patent/JP2003527423A/ja active Pending
- 2001-02-20 CA CA002400637A patent/CA2400637A1/en not_active Abandoned
- 2001-02-23 BR BR0109230-8A patent/BR0109230A/pt not_active Application Discontinuation
- 2001-02-23 AU AU2001245310A patent/AU2001245310B2/en not_active Ceased
- 2001-02-23 PT PT01918208T patent/PT1263504E/pt unknown
- 2001-02-23 KR KR1020027012171A patent/KR20030009390A/ko not_active Withdrawn
- 2001-02-23 JP JP2001568420A patent/JP4789231B2/ja not_active Expired - Fee Related
- 2001-02-23 DK DK01918208T patent/DK1263504T3/da active
- 2001-02-23 AU AU2001239836A patent/AU2001239836A1/en not_active Abandoned
- 2001-02-23 ES ES01918208T patent/ES2204848T3/es not_active Expired - Lifetime
- 2001-02-23 PL PL358306A patent/PL203709B1/pl not_active IP Right Cessation
- 2001-02-23 CA CA002399985A patent/CA2399985A1/en not_active Abandoned
- 2001-02-23 EP EP01914447A patent/EP1267878A2/en not_active Withdrawn
- 2001-02-23 AT AT01918208T patent/ATE247507T1/de active
- 2001-02-23 WO PCT/US2001/005740 patent/WO2001070230A2/en not_active Ceased
- 2001-02-23 CA CA2400639A patent/CA2400639C/en not_active Expired - Fee Related
- 2001-02-23 MX MXPA02009072A patent/MXPA02009072A/es active IP Right Grant
- 2001-02-23 EP EP01918208A patent/EP1263504B1/en not_active Expired - Lifetime
- 2001-02-23 AU AU4531001A patent/AU4531001A/xx active Pending
- 2001-02-23 WO PCT/US2001/005700 patent/WO2001070222A2/en not_active Ceased
- 2001-02-23 JP JP2001568428A patent/JP2003527427A/ja not_active Withdrawn
- 2001-02-23 BR BR0109211-1A patent/BR0109211A/pt not_active Application Discontinuation
- 2001-02-23 KR KR1020027012170A patent/KR100749191B1/ko not_active Expired - Fee Related
- 2001-02-23 MX MXPA02009073A patent/MXPA02009073A/es unknown
- 2001-02-23 CN CN01806620A patent/CN1418100A/zh active Pending
- 2001-02-23 CN CNB018067646A patent/CN1198605C/zh not_active Expired - Fee Related
- 2001-02-23 DE DE60100625T patent/DE60100625T2/de not_active Expired - Lifetime
- 2001-03-15 AR ARP010101211A patent/AR028258A1/es not_active Application Discontinuation
- 2001-03-16 TW TW090106235A patent/TWI268777B/zh not_active IP Right Cessation
-
2002
- 2002-08-08 ZA ZA200206350A patent/ZA200206350B/en unknown
-
2005
- 2005-06-15 AU AU2005202600A patent/AU2005202600B2/en not_active Ceased
-
2010
- 2010-11-24 JP JP2010261857A patent/JP2011037901A/ja not_active Withdrawn
-
2011
- 2011-05-13 JP JP2011108785A patent/JP2011153158A/ja not_active Withdrawn
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MXPA02009071A (es) | Compuestos con actividad agonista de 5-ht 1a para tratar glaucoma.. | |
| EP1112106A2 (en) | Serotonergic 5ht2 agonists for treating glaucoma | |
| US20040106597A1 (en) | Novel fused indazoles and indoles and their use for the treatment of glaucoma | |
| KR20050074547A (ko) | 눈의 퇴행성 질환을 치료하기 위한 히스톤 디아세틸라제저해제 | |
| US20040110791A1 (en) | Novel arylaminopropane analogues and their use for the treatment of glaucoma | |
| US7208512B2 (en) | Benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma | |
| Saxena et al. | Pharmacotherapy of glaucoma | |
| US20030114512A1 (en) | Compounds with 5-ht2 and 5-ht1a agonist activity for treating glaucoma | |
| MXPA05002259A (es) | Compuestos de 5-croman-5-il-etilamina sustituidos y uso para el tratamiento de glaucoma. | |
| EP1268482B1 (en) | Pyranoindoles for treating glaucoma | |
| MXPA05006277A (es) | Analogos de benzopirano novedosos y su uso para el tratamiento de glaucoma. | |
| WO2007090134A2 (en) | Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma | |
| US20030119846A1 (en) | Compounds with 5-ht activity useful for controlling visual field loss | |
| EP1859795A1 (en) | Therapeutic agent for ophthalmic disease | |
| US20060211700A1 (en) | (R)-8,9-dichloro-2,3,4,4a-tetrahydro-1H,6H-pyrazino[1,2-a]quinoxalin-5-one for controlling IOP and treating glaucoma | |
| MXPA01002697A (en) | Serotonergic 5ht2 | |
| AU2004214563A1 (en) | Combination therapy for treating glaucoma | |
| HK1050897B (en) | Pyranoindoles for treating glaucoma |