ZA200208776B - Daily treatment for erectile dysfunction using a PDE5 innhibitor. - Google Patents
Daily treatment for erectile dysfunction using a PDE5 innhibitor. Download PDFInfo
- Publication number
- ZA200208776B ZA200208776B ZA200208776A ZA200208776A ZA200208776B ZA 200208776 B ZA200208776 B ZA 200208776B ZA 200208776 A ZA200208776 A ZA 200208776A ZA 200208776 A ZA200208776 A ZA 200208776A ZA 200208776 B ZA200208776 B ZA 200208776B
- Authority
- ZA
- South Africa
- Prior art keywords
- inhibitor
- methyl
- pde5
- article
- pdes
- Prior art date
Links
- 101100189582 Dictyostelium discoideum pdeD gene Proteins 0.000 title claims 3
- 101150098694 PDE5A gene Proteins 0.000 title claims 3
- 102100029175 cGMP-specific 3',5'-cyclic phosphodiesterase Human genes 0.000 title claims 3
- 201000001881 impotence Diseases 0.000 title description 12
- 208000010228 Erectile Dysfunction Diseases 0.000 title description 11
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims description 50
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims description 50
- 239000003112 inhibitor Substances 0.000 claims description 43
- 230000001684 chronic effect Effects 0.000 claims description 40
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims description 38
- 101150085511 PEDS1 gene Proteins 0.000 claims description 27
- 102100037592 Plasmanylethanolamine desaturase Human genes 0.000 claims description 27
- 229920003199 poly(diethylsiloxane) Polymers 0.000 claims description 27
- 238000004519 manufacturing process Methods 0.000 claims description 23
- 201000001880 Sexual dysfunction Diseases 0.000 claims description 17
- 230000005764 inhibitory process Effects 0.000 claims description 17
- 239000006186 oral dosage form Substances 0.000 claims description 17
- 231100000872 sexual dysfunction Toxicity 0.000 claims description 17
- 229960003310 sildenafil Drugs 0.000 claims description 17
- 230000003750 conditioning effect Effects 0.000 claims description 14
- 230000002792 vascular Effects 0.000 claims description 14
- -1 3,4- methylenedioxyphenyl Chemical group 0.000 claims description 9
- 101100351286 Dictyostelium discoideum pdeE gene Proteins 0.000 claims description 9
- SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 claims description 9
- 230000001154 acute effect Effects 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- 101150037969 pde-6 gene Proteins 0.000 claims description 9
- 229960002381 vardenafil Drugs 0.000 claims description 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 210000005226 corpus cavernosum Anatomy 0.000 claims description 5
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 3
- 239000002249 anxiolytic agent Substances 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 210000002460 smooth muscle Anatomy 0.000 claims description 2
- GFVZTCIYHIUUJO-UHFFFAOYSA-N 5-[2-ethoxy-5-(1-methylimidazol-2-yl)phenyl]-1-methyl-3-propyl-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1C1=NC=CN1C GFVZTCIYHIUUJO-UHFFFAOYSA-N 0.000 claims 1
- 102000011016 Type 5 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 description 17
- 108010037581 Type 5 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 description 17
- 125000000217 alkyl group Chemical group 0.000 description 12
- 239000002552 dosage form Substances 0.000 description 12
- 150000001875 compounds Chemical class 0.000 description 9
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 description 8
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 description 8
- 239000000825 pharmaceutical preparation Substances 0.000 description 8
- 229940127557 pharmaceutical product Drugs 0.000 description 8
- 230000001568 sexual effect Effects 0.000 description 8
- 239000003826 tablet Substances 0.000 description 8
- 239000000047 product Substances 0.000 description 7
- 229940079593 drug Drugs 0.000 description 6
- 239000001257 hydrogen Substances 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 239000007787 solid Substances 0.000 description 6
- 229910052736 halogen Inorganic materials 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 238000002560 therapeutic procedure Methods 0.000 description 5
- NYHBQMYGNKIUIF-UUOKFMHZSA-N Guanosine Chemical compound C1=NC=2C(=O)NC(N)=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O NYHBQMYGNKIUIF-UUOKFMHZSA-N 0.000 description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 230000008901 benefit Effects 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 description 3
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 230000001419 dependent effect Effects 0.000 description 3
- 239000007888 film coating Substances 0.000 description 3
- 238000009501 film coating Methods 0.000 description 3
- 239000007903 gelatin capsule Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 230000004044 response Effects 0.000 description 3
- 102100034044 All-trans-retinol dehydrogenase [NAD(+)] ADH1B Human genes 0.000 description 2
- 101710193111 All-trans-retinol dehydrogenase [NAD(+)] ADH4 Proteins 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- MIKUYHXYGGJMLM-GIMIYPNGSA-N Crotonoside Natural products C1=NC2=C(N)NC(=O)N=C2N1[C@H]1O[C@@H](CO)[C@H](O)[C@@H]1O MIKUYHXYGGJMLM-GIMIYPNGSA-N 0.000 description 2
- NYHBQMYGNKIUIF-UHFFFAOYSA-N D-guanosine Natural products C1=2NC(N)=NC(=O)C=2N=CN1C1OC(CO)C(O)C1O NYHBQMYGNKIUIF-UHFFFAOYSA-N 0.000 description 2
- 101100135868 Dictyostelium discoideum pde3 gene Proteins 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 2
- 108700007698 Genetic Terminator Regions Proteins 0.000 description 2
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 description 2
- 230000005856 abnormality Effects 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 125000003342 alkenyl group Chemical group 0.000 description 2
- 125000003545 alkoxy group Chemical group 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 230000009286 beneficial effect Effects 0.000 description 2
- 125000002619 bicyclic group Chemical group 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 238000007906 compression Methods 0.000 description 2
- 230000006835 compression Effects 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- VHJLVAABSRFDPM-QWWZWVQMSA-N dithiothreitol Chemical compound SC[C@@H](O)[C@H](O)CS VHJLVAABSRFDPM-QWWZWVQMSA-N 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000004438 eyesight Effects 0.000 description 2
- 238000011010 flushing procedure Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000007897 gelcap Substances 0.000 description 2
- 229940029575 guanosine Drugs 0.000 description 2
- 150000002431 hydrogen Chemical class 0.000 description 2
- 239000012669 liquid formulation Substances 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000003801 milling Methods 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 230000004043 responsiveness Effects 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 239000007909 solid dosage form Substances 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 238000013268 sustained release Methods 0.000 description 2
- 239000012730 sustained-release form Substances 0.000 description 2
- 229940094720 viagra Drugs 0.000 description 2
- FQVLRGLGWNWPSS-BXBUPLCLSA-N (4r,7s,10s,13s,16r)-16-acetamido-13-(1h-imidazol-5-ylmethyl)-10-methyl-6,9,12,15-tetraoxo-7-propan-2-yl-1,2-dithia-5,8,11,14-tetrazacycloheptadecane-4-carboxamide Chemical compound N1C(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@@H]1CC1=CN=CN1 FQVLRGLGWNWPSS-BXBUPLCLSA-N 0.000 description 1
- DDQVAJSWFPJSGC-UHFFFAOYSA-N 5-[5-[4-(2-hydroxyethyl)piperazin-1-yl]sulfonyl-2-propoxyphenyl]-1-methyl-3-propyl-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound C1=C(C=2NC=3C(CCC)=NN(C)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)N1CCN(CCO)CC1 DDQVAJSWFPJSGC-UHFFFAOYSA-N 0.000 description 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- 102100034035 Alcohol dehydrogenase 1A Human genes 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 239000007989 BIS-Tris Propane buffer Substances 0.000 description 1
- 101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 description 1
- 101100135859 Dictyostelium discoideum regA gene Proteins 0.000 description 1
- 208000021663 Female sexual arousal disease Diseases 0.000 description 1
- 206010016825 Flushing Diseases 0.000 description 1
- 101000892220 Geobacillus thermodenitrificans (strain NG80-2) Long-chain-alcohol dehydrogenase 1 Proteins 0.000 description 1
- 101000780443 Homo sapiens Alcohol dehydrogenase 1A Proteins 0.000 description 1
- 101100296723 Homo sapiens PDE5A gene Proteins 0.000 description 1
- 101100351296 Homo sapiens PEDS1 gene Proteins 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 101100082606 Plasmodium falciparum (isolate 3D7) PDEbeta gene Proteins 0.000 description 1
- 101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 239000012564 Q sepharose fast flow resin Substances 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 241000235070 Saccharomyces Species 0.000 description 1
- 101100135860 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) PDE2 gene Proteins 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 239000005864 Sulphur Chemical group 0.000 description 1
- 206010047571 Visual impairment Diseases 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- PXXJHWLDUBFPOL-UHFFFAOYSA-N benzamidine Chemical compound NC(=N)C1=CC=CC=C1 PXXJHWLDUBFPOL-UHFFFAOYSA-N 0.000 description 1
- HHKZCCWKTZRCCL-UHFFFAOYSA-N bis-tris propane Chemical compound OCC(CO)(CO)NCCCNC(CO)(CO)CO HHKZCCWKTZRCCL-UHFFFAOYSA-N 0.000 description 1
- 230000001271 cGMP hydrolyzing effect Effects 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 235000010216 calcium carbonate Nutrition 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 230000005794 circulatory dysfunction Effects 0.000 description 1
- 230000007012 clinical effect Effects 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 230000004456 color vision Effects 0.000 description 1
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 239000002532 enzyme inhibitor Substances 0.000 description 1
- 230000001856 erectile effect Effects 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 239000011888 foil Substances 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 235000021472 generally recognized as safe Nutrition 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 230000002439 hemostatic effect Effects 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 229910052588 hydroxylapatite Inorganic materials 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000006166 lysate Substances 0.000 description 1
- 239000012139 lysis buffer Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 150000002739 metals Chemical class 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000007932 molded tablet Substances 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 210000002464 muscle smooth vascular Anatomy 0.000 description 1
- 229910052757 nitrogen Chemical group 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 239000013612 plasmid Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000000391 smoking effect Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 230000004865 vascular response Effects 0.000 description 1
- 210000005166 vasculature Anatomy 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
- 230000004393 visual impairment Effects 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 238000005550 wet granulation 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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Plant Substances (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/558,911 US6451807B1 (en) | 1999-04-30 | 2000-04-26 | Methods of treating sexual dysfunction in an individual suffering from a retinal disease, class 1 congestive heart failure, or myocardial infarction using a PDE5 inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200208776B true ZA200208776B (en) | 2003-06-03 |
Family
ID=24231497
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200208776A ZA200208776B (en) | 2000-04-26 | 2002-10-30 | Daily treatment for erectile dysfunction using a PDE5 innhibitor. |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US6451807B1 (fr) |
| EP (1) | EP1276481A2 (fr) |
| JP (1) | JP2003531174A (fr) |
| KR (1) | KR20030007551A (fr) |
| CN (1) | CN1446091A (fr) |
| AU (1) | AU2001253612A1 (fr) |
| BR (1) | BR0110373A (fr) |
| CA (1) | CA2407519A1 (fr) |
| CZ (1) | CZ20023577A3 (fr) |
| EA (1) | EA200201011A1 (fr) |
| HR (1) | HRP20020827A2 (fr) |
| HU (1) | HUP0300477A3 (fr) |
| IL (1) | IL152227A0 (fr) |
| MX (1) | MXPA02010539A (fr) |
| NO (1) | NO20025138L (fr) |
| NZ (1) | NZ521869A (fr) |
| PL (1) | PL360186A1 (fr) |
| SK (1) | SK15392002A3 (fr) |
| WO (1) | WO2001080860A2 (fr) |
| ZA (1) | ZA200208776B (fr) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060222647A1 (en) * | 1993-05-27 | 2006-10-05 | Beavo Joseph A | Methods and compositions for modulating the activity of PDE5 |
| IL135817A0 (en) * | 1999-04-30 | 2001-05-20 | Lilly Icos Llc | Phosphodiesterase enzyme inhibitors and their use in pharmaceutical articles |
| US6943166B1 (en) * | 1999-04-30 | 2005-09-13 | Lilly Icos Llc. | Compositions comprising phosphodiesterase inhabitors for the treatment of sexual disfunction |
| AU2001257146B2 (en) * | 2000-04-19 | 2006-11-30 | Johns Hopkins University | Methods for prevention and treatment of gastrointestinal disorders |
| US8133903B2 (en) * | 2003-10-21 | 2012-03-13 | Los Angeles Biomedical Research Institute at Harbor—UCLA Medical Center | Methods of use of inhibitors of phosphodiesterases and modulators of nitric oxide, reactive oxygen species, and metalloproteinases in the treatment of peyronie's disease, arteriosclerosis and other fibrotic diseases |
| US20050048573A1 (en) * | 2003-02-03 | 2005-03-03 | Plexxikon, Inc. | PDE5A crystal structure and uses |
| CN101106997A (zh) * | 2004-08-17 | 2008-01-16 | 约翰·霍普金斯大学 | Pde5抑制剂组合物及治疗心脏病征候的方法 |
| US20060205733A1 (en) * | 2004-08-26 | 2006-09-14 | Encysive Pharmaceuticals | Endothelin a receptor antagonists in combination with phosphodiesterase 5 inhibitors and uses thereof |
| US7265248B1 (en) | 2005-04-29 | 2007-09-04 | Technology Innovations, Llc | Compositions and methods for the treatment of malaria |
| WO2007100387A2 (fr) * | 2005-11-03 | 2007-09-07 | Dr. Reddy's Laboratories Ltd. | Procédé de préparation de tadalafil |
| US20100324037A1 (en) * | 2006-08-24 | 2010-12-23 | Surface Logix, Inc. | Pharmacokinetically improved compounds |
| TWI462923B (zh) * | 2010-10-18 | 2014-12-01 | Univ Kaohsiung Medical | Ｋｍｕｐ－３之心肌梗塞疾患用途 |
| WO2017168174A1 (fr) | 2016-04-02 | 2017-10-05 | N4 Pharma Uk Limited | Nouvelles formes pharmaceutiques du sildénafil |
| JP6578046B1 (ja) * | 2018-08-23 | 2019-09-18 | Ｔｏｗａ Ｃｏｒｐｏｒａｔｉｏｎ 株式会社 | Ｐｄｅ５阻害用医薬組成物及びｐｄｅ５阻害用食品組成物 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4931445A (en) | 1988-10-06 | 1990-06-05 | Irwin Goldstein | Agents for treatment of male impotence |
| NZ234186A (en) | 1989-07-07 | 1991-10-25 | Janssen Pharmaceutica Nv | Imidazo quinazolin-one derivatives and pharmaceutical compositions |
| EP1038963B1 (fr) | 1993-05-27 | 2009-08-05 | Board Of Regents Of The University Of Washington | Phosphodiésterase de fixation du monophosphate de guanosine cyclique et avec specificité pour celui-ci et procédé d'obtention |
| GB9301192D0 (en) * | 1993-06-09 | 1993-06-09 | Trott Francis W | Flower shaped mechanised table |
| GB9514465D0 (en) | 1995-07-14 | 1995-09-13 | Glaxo Lab Sa | Chemical compounds |
| GB9401090D0 (en) | 1994-01-21 | 1994-03-16 | Glaxo Lab Sa | Chemical compounds |
| GB9511220D0 (en) | 1995-06-02 | 1995-07-26 | Glaxo Group Ltd | Solid dispersions |
| GB9514464D0 (en) * | 1995-07-14 | 1995-09-13 | Glaxo Lab Sa | Medicaments |
| GB9514473D0 (en) | 1995-07-14 | 1995-09-13 | Glaxo Lab Sa | Chemical compounds |
| IL126951A0 (en) | 1996-05-10 | 1999-09-22 | Icos Corp | Carboline derivatives |
| CA2339630C (fr) | 1998-09-16 | 2006-05-23 | Icos Corporation | Derives de carboline en tant qu'inhibiteurs de la gmp cyclique phosphodiesterase |
-
2000
- 2000-04-26 US US09/558,911 patent/US6451807B1/en not_active Expired - Fee Related
-
2001
- 2001-04-13 CN CN01811844A patent/CN1446091A/zh active Pending
- 2001-04-13 MX MXPA02010539A patent/MXPA02010539A/es unknown
- 2001-04-13 HU HU0300477A patent/HUP0300477A3/hu unknown
- 2001-04-13 SK SK1539-2002A patent/SK15392002A3/sk unknown
- 2001-04-13 EA EA200201011A patent/EA200201011A1/ru unknown
- 2001-04-13 NZ NZ521869A patent/NZ521869A/en unknown
- 2001-04-13 KR KR1020027014383A patent/KR20030007551A/ko not_active Application Discontinuation
- 2001-04-13 IL IL15222701A patent/IL152227A0/xx unknown
- 2001-04-13 CZ CZ20023577A patent/CZ20023577A3/cs unknown
- 2001-04-13 EP EP01927133A patent/EP1276481A2/fr not_active Withdrawn
- 2001-04-13 WO PCT/US2001/012512 patent/WO2001080860A2/fr not_active Application Discontinuation
- 2001-04-13 BR BR0110373-3A patent/BR0110373A/pt not_active IP Right Cessation
- 2001-04-13 JP JP2001577959A patent/JP2003531174A/ja not_active Withdrawn
- 2001-04-13 CA CA002407519A patent/CA2407519A1/fr not_active Abandoned
- 2001-04-13 PL PL36018601A patent/PL360186A1/xx not_active Application Discontinuation
- 2001-04-13 AU AU2001253612A patent/AU2001253612A1/en not_active Abandoned
-
2002
- 2002-07-19 US US10/198,903 patent/US20030100478A1/en not_active Abandoned
- 2002-10-16 HR HRP20020827 patent/HRP20020827A2/hr not_active Application Discontinuation
- 2002-10-25 NO NO20025138A patent/NO20025138L/no not_active Application Discontinuation
- 2002-10-30 ZA ZA200208776A patent/ZA200208776B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SK15392002A3 (sk) | 2003-03-04 |
| MXPA02010539A (es) | 2003-05-14 |
| NZ521869A (en) | 2004-10-29 |
| BR0110373A (pt) | 2003-02-18 |
| KR20030007551A (ko) | 2003-01-23 |
| CA2407519A1 (fr) | 2001-11-01 |
| WO2001080860A3 (fr) | 2002-06-06 |
| NO20025138L (no) | 2002-12-16 |
| IL152227A0 (en) | 2003-05-29 |
| CN1446091A (zh) | 2003-10-01 |
| US20030100478A1 (en) | 2003-05-29 |
| NO20025138D0 (no) | 2002-10-25 |
| AU2001253612A1 (en) | 2001-11-07 |
| PL360186A1 (en) | 2004-09-06 |
| EA200201011A1 (ru) | 2003-06-26 |
| US6451807B1 (en) | 2002-09-17 |
| CZ20023577A3 (cs) | 2003-06-18 |
| HUP0300477A3 (en) | 2004-10-28 |
| EP1276481A2 (fr) | 2003-01-22 |
| WO2001080860A2 (fr) | 2001-11-01 |
| JP2003531174A (ja) | 2003-10-21 |
| HUP0300477A2 (hu) | 2003-06-28 |
| HRP20020827A2 (en) | 2004-12-31 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200208776B (en) | Daily treatment for erectile dysfunction using a PDE5 innhibitor. | |
| US20040058929A1 (en) | Unit dosage form | |
| KR100577057B1 (ko) | 단위 제형 | |
| US20030144296A1 (en) | Daily treatment for erectile dysfunction using a PDE5 inhibitor | |
| TW200407153A (en) | Novel combination | |
| AU2003242895A1 (en) | Combination of PDE5 inhibitors with angiotensin II receptor antagonists | |
| CA2203379C (fr) | Inhibiteurs de cgmp-pde destines au traitement du dysfonctionnement erectile | |
| TW201240994A (en) | Composition for reducing skin wrinkles including PDE5 inhibitor | |
| MXPA00009614A (en) | Combination effective for the treatment of impotence comprising a potassium-channel-opener and a cgmp elevator |