SK8782000A3 - Combination, composition and kits effective for the treatment of impotence - Google Patents

Combination, composition and kits effective for the treatment of impotence Download PDF

Info

Publication number: SK8782000A3
Authority: SK; Slovakia
Prior art keywords: compound; pharmaceutically acceptable; impotence; composition; medicament
Prior art date: 1997-12-16

Application number

SK878-2000A

Other languages

English (en)

Slovak (sk)

Inventor

Michael Grant Wyllie

Original Assignee

Pfizer Prod Inc

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1997-12-16

Filing date

1998-10-29

Publication date

2002-03-05

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22090927&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SK8782000(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1998-10-29 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2002-03-05 Publication of SK8782000A3 publication Critical patent/SK8782000A3/sk

Links

201000001881 impotence Diseases 0.000 title claims abstract description 82
239000000203 mixture Substances 0.000 title claims abstract description 82
150000001875 compounds Chemical class 0.000 claims abstract description 194
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 claims abstract description 118
150000003839 salts Chemical class 0.000 claims abstract description 78
239000000674 adrenergic antagonist Substances 0.000 claims abstract description 62
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 abstract description 44
229960003310 sildenafil Drugs 0.000 claims abstract description 21
208000010228 Erectile Dysfunction Diseases 0.000 claims abstract description 8
239000003814 drug Substances 0.000 claims description 56
229940099471 Phosphodiesterase inhibitor Drugs 0.000 claims description 52
125000004432 carbon atom Chemical group C* 0.000 claims description 45
239000005557 antagonist Substances 0.000 claims description 41
-1 C 1 -C 6 alkyl Chemical group 0.000 claims description 38
RUZYUOTYCVRMRZ-UHFFFAOYSA-N doxazosin Chemical compound C1OC2=CC=CC=C2OC1C(=O)N(CC1)CCN1C1=NC(N)=C(C=C(C(OC)=C2)OC)C2=N1 RUZYUOTYCVRMRZ-UHFFFAOYSA-N 0.000 claims description 38
229960001389 doxazosin Drugs 0.000 claims description 38
UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims description 36
229910052739 hydrogen Inorganic materials 0.000 claims description 30
239000001257 hydrogen Substances 0.000 claims description 29
YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 24
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 24
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 24
125000000217 alkyl group Chemical group 0.000 claims description 23
150000002431 hydrogen Chemical class 0.000 claims description 23
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 21
229960001289 prazosin Drugs 0.000 claims description 21
IENZQIKPVFGBNW-UHFFFAOYSA-N prazosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(CC1)CCN1C(=O)C1=CC=CO1 IENZQIKPVFGBNW-UHFFFAOYSA-N 0.000 claims description 21
VCKUSRYTPJJLNI-UHFFFAOYSA-N terazosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(CC1)CCN1C(=O)C1CCCO1 VCKUSRYTPJJLNI-UHFFFAOYSA-N 0.000 claims description 21
229960001693 terazosin Drugs 0.000 claims description 20
DEIYFTQMQPDXOT-UHFFFAOYSA-N sildenafil citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 DEIYFTQMQPDXOT-UHFFFAOYSA-N 0.000 claims description 14
230000002195 synergetic effect Effects 0.000 claims description 14
108010044467 Isoenzymes Proteins 0.000 claims description 13
239000003085 diluting agent Substances 0.000 claims description 13
239000002552 dosage form Substances 0.000 claims description 13
125000005842 heteroatom Chemical group 0.000 claims description 13
239000012453 solvate Substances 0.000 claims description 13
AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 12
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 12
125000003118 aryl group Chemical group 0.000 claims description 12
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 12
125000002619 bicyclic group Chemical group 0.000 claims description 12
RFWZESUMWJKKRN-UHFFFAOYSA-N dapiprazole Chemical compound CC1=CC=CC=C1N1CCN(CCC=2N3CCCCC3=NN=2)CC1 RFWZESUMWJKKRN-UHFFFAOYSA-N 0.000 claims description 12
229960002947 dapiprazole Drugs 0.000 claims description 12
229910052736 halogen Inorganic materials 0.000 claims description 12
150000002367 halogens Chemical class 0.000 claims description 12
125000004446 heteroarylalkyl group Chemical group 0.000 claims description 12
125000002950 monocyclic group Chemical group 0.000 claims description 12
229910052760 oxygen Inorganic materials 0.000 claims description 12
239000001301 oxygen Substances 0.000 claims description 12
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 12
229920006395 saturated elastomer Polymers 0.000 claims description 12
229910052717 sulfur Inorganic materials 0.000 claims description 12
239000011593 sulfur Chemical group 0.000 claims description 12
229930192474 thiophene Natural products 0.000 claims description 12
125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 11
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 11
102000015007 alpha-adrenergic receptor activity proteins Human genes 0.000 claims description 11
108040006816 alpha-adrenergic receptor activity proteins Proteins 0.000 claims description 11
VJECBOKJABCYMF-UHFFFAOYSA-N doxazosin mesylate Chemical group [H+].CS([O-])(=O)=O.C1OC2=CC=CC=C2OC1C(=O)N(CC1)CCN1C1=NC(N)=C(C=C(C(OC)=C2)OC)C2=N1 VJECBOKJABCYMF-UHFFFAOYSA-N 0.000 claims description 11
239000003937 drug carrier Substances 0.000 claims description 11
229910052757 nitrogen Chemical group 0.000 claims description 11
MRBDMNSDAVCSSF-UHFFFAOYSA-N phentolamine Chemical compound C1=CC(C)=CC=C1N(C=1C=C(O)C=CC=1)CC1=NCCN1 MRBDMNSDAVCSSF-UHFFFAOYSA-N 0.000 claims description 11
229960001999 phentolamine Drugs 0.000 claims description 11
PHLBKPHSAVXXEF-UHFFFAOYSA-N trazodone Chemical compound ClC1=CC=CC(N2CCN(CCCN3C(N4C=CC=CC4=N3)=O)CC2)=C1 PHLBKPHSAVXXEF-UHFFFAOYSA-N 0.000 claims description 11
229960003991 trazodone Drugs 0.000 claims description 11
206010057671 Female sexual dysfunction Diseases 0.000 claims description 10
229960002639 sildenafil citrate Drugs 0.000 claims description 10
SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 10
JXZZEXZZKAWDSP-UHFFFAOYSA-N 3-(2-(4-Benzamidopiperid-1-yl)ethyl)indole Chemical compound C1CN(CCC=2C3=CC=CC=C3NC=2)CCC1NC(=O)C1=CC=CC=C1 JXZZEXZZKAWDSP-UHFFFAOYSA-N 0.000 claims description 9
QZVCTJOXCFMACW-UHFFFAOYSA-N Phenoxybenzamine Chemical compound C=1C=CC=CC=1CN(CCCl)C(C)COC1=CC=CC=C1 QZVCTJOXCFMACW-UHFFFAOYSA-N 0.000 claims description 9
DRHKJLXJIQTDTD-OAHLLOKOSA-N Tamsulosine Chemical compound CCOC1=CC=CC=C1OCCN[C@H](C)CC1=CC=C(OC)C(S(N)(=O)=O)=C1 DRHKJLXJIQTDTD-OAHLLOKOSA-N 0.000 claims description 9
WNMJYKCGWZFFKR-UHFFFAOYSA-N alfuzosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(C)CCCNC(=O)C1CCCO1 WNMJYKCGWZFFKR-UHFFFAOYSA-N 0.000 claims description 9
229960004607 alfuzosin Drugs 0.000 claims description 9
230000003028 elevating effect Effects 0.000 claims description 9
HPMRFMKYPGXPEP-UHFFFAOYSA-N idazoxan Chemical compound N1CCN=C1C1OC2=CC=CC=C2OC1 HPMRFMKYPGXPEP-UHFFFAOYSA-N 0.000 claims description 9
229960002056 indoramin Drugs 0.000 claims description 9
229960003418 phenoxybenzamine Drugs 0.000 claims description 9
229960002613 tamsulosin Drugs 0.000 claims description 9
230000001225 therapeutic effect Effects 0.000 claims description 8
125000003710 aryl alkyl group Chemical group 0.000 claims description 7
150000003180 prostaglandins Chemical class 0.000 claims description 7
125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 6
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
BLGXFZZNTVWLAY-CCZXDCJGSA-N Yohimbine Natural products C1=CC=C2C(CCN3C[C@@H]4CC[C@@H](O)[C@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-CCZXDCJGSA-N 0.000 claims description 6
BLGXFZZNTVWLAY-UHFFFAOYSA-N beta-Yohimbin Natural products C1=CC=C2C(CCN3CC4CCC(O)C(C4CC33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-UHFFFAOYSA-N 0.000 claims description 6
125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 6
229960000317 yohimbine Drugs 0.000 claims description 6
AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 0.000 claims description 6
125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 5
239000002160 alpha blocker Substances 0.000 claims description 5
KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical group [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 4
230000002301 combined effect Effects 0.000 claims description 4
238000004806 packaging method and process Methods 0.000 claims description 4
230000002708 enhancing effect Effects 0.000 claims description 3
125000003342 alkenyl group Chemical group 0.000 claims 5
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical group OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 5
125000000753 cycloalkyl group Chemical group 0.000 claims 4
BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 claims 4
ANZIISNSHPKVRV-UHFFFAOYSA-N abanoquil Chemical compound C1=C(OC)C(OC)=CC2=NC(N3CCC=4C=C(C(=CC=4C3)OC)OC)=CC(N)=C21 ANZIISNSHPKVRV-UHFFFAOYSA-N 0.000 claims 3
229950010137 abanoquil Drugs 0.000 claims 3
NRNCYVBFPDDJNE-UHFFFAOYSA-N pemoline Chemical compound O1C(N)=NC(=O)C1C1=CC=CC=C1 NRNCYVBFPDDJNE-UHFFFAOYSA-N 0.000 claims 2
229960000761 pemoline Drugs 0.000 claims 2
PKRSYEPBQPFNRB-UHFFFAOYSA-N 2-phenoxybenzoic acid Chemical compound OC(=O)C1=CC=CC=C1OC1=CC=CC=C1 PKRSYEPBQPFNRB-UHFFFAOYSA-N 0.000 claims 1
239000000951 adrenergic alpha-1 receptor antagonist Substances 0.000 claims 1
239000002876 beta blocker Substances 0.000 claims 1
229910052799 carbon Inorganic materials 0.000 claims 1
238000004519 manufacturing process Methods 0.000 claims 1
239000003795 chemical substances by application Substances 0.000 abstract description 8
102000004305 alpha Adrenergic Receptors Human genes 0.000 abstract description 5
108090000861 alpha Adrenergic Receptors Proteins 0.000 abstract description 5
ZOOGRGPOEVQQDX-UHFFFAOYSA-N cyclic GMP Natural products O1C2COP(O)(=O)OC2C(O)C1N1C=NC2=C1NC(N)=NC2=O ZOOGRGPOEVQQDX-UHFFFAOYSA-N 0.000 description 48
230000000694 effects Effects 0.000 description 24
239000003826 tablet Substances 0.000 description 21
239000002775 capsule Substances 0.000 description 13
238000011260 co-administration Methods 0.000 description 11
239000003112 inhibitor Substances 0.000 description 10
210000003899 penis Anatomy 0.000 description 8
239000000243 solution Substances 0.000 description 8
102000004861 Phosphoric Diester Hydrolases Human genes 0.000 description 6
108090001050 Phosphoric Diester Hydrolases Proteins 0.000 description 6
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
238000000034 method Methods 0.000 description 6
239000008194 pharmaceutical composition Substances 0.000 description 6
238000012360 testing method Methods 0.000 description 6
239000007924 injection Substances 0.000 description 5
238000002347 injection Methods 0.000 description 5
210000001519 tissue Anatomy 0.000 description 5
SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 4
241001465754 Metazoa Species 0.000 description 4
239000007864 aqueous solution Substances 0.000 description 4
210000004027 cell Anatomy 0.000 description 4
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
229940079593 drug Drugs 0.000 description 4
239000004615 ingredient Substances 0.000 description 4
229960002748 norepinephrine Drugs 0.000 description 4
SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 4
108060003345 Adrenergic Receptor Proteins 0.000 description 3
102000017910 Adrenergic receptor Human genes 0.000 description 3
241000282693 Cercopithecidae Species 0.000 description 3
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
241000124008 Mammalia Species 0.000 description 3
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
239000004480 active ingredient Substances 0.000 description 3
230000000996 additive effect Effects 0.000 description 3
239000000556 agonist Substances 0.000 description 3
230000008602 contraction Effects 0.000 description 3
230000004064 dysfunction Effects 0.000 description 3
239000000463 material Substances 0.000 description 3
230000007246 mechanism Effects 0.000 description 3
239000002858 neurotransmitter agent Substances 0.000 description 3
239000006187 pill Substances 0.000 description 3
102000005962 receptors Human genes 0.000 description 3
108020003175 receptors Proteins 0.000 description 3
230000001568 sexual effect Effects 0.000 description 3
230000036332 sexual response Effects 0.000 description 3
238000012546 transfer Methods 0.000 description 3
CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 description 2
LDORHCBMWSQLIU-UHFFFAOYSA-N 6-phenyl-1h-pyrimidin-2-one Chemical class N1C(=O)N=CC=C1C1=CC=CC=C1 LDORHCBMWSQLIU-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
241000282472 Canis lupus familiaris Species 0.000 description 2
GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 description 2
102000004190 Enzymes Human genes 0.000 description 2
108090000790 Enzymes Proteins 0.000 description 2
206010020772 Hypertension Diseases 0.000 description 2
206010022086 Injection site pain Diseases 0.000 description 2
229940124639 Selective inhibitor Drugs 0.000 description 2
201000001880 Sexual dysfunction Diseases 0.000 description 2
229920002472 Starch Polymers 0.000 description 2
230000009471 action Effects 0.000 description 2
239000000654 additive Substances 0.000 description 2
229930013930 alkaloid Natural products 0.000 description 2
239000008280 blood Substances 0.000 description 2
210000004369 blood Anatomy 0.000 description 2
RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 2
150000001860 citric acid derivatives Chemical class 0.000 description 2
229960002896 clonidine Drugs 0.000 description 2
201000010099 disease Diseases 0.000 description 2
208000035475 disorder Diseases 0.000 description 2
230000001856 erectile effect Effects 0.000 description 2
230000009986 erectile function Effects 0.000 description 2
239000011888 foil Substances 0.000 description 2
230000001939 inductive effect Effects 0.000 description 2
239000007926 intracavernous injection Substances 0.000 description 2
238000007915 intraurethral administration Methods 0.000 description 2
230000007774 longterm Effects 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
239000012528 membrane Substances 0.000 description 2
229940094443 oxytocics prostaglandins Drugs 0.000 description 2
XQYZDYMELSJDRZ-UHFFFAOYSA-N papaverine Chemical compound C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 XQYZDYMELSJDRZ-UHFFFAOYSA-N 0.000 description 2
229920003023 plastic Polymers 0.000 description 2
239000002985 plastic film Substances 0.000 description 2
229920006255 plastic film Polymers 0.000 description 2
201000011264 priapism Diseases 0.000 description 2
150000003230 pyrimidines Chemical class 0.000 description 2
150000003246 quinazolines Chemical class 0.000 description 2
230000004044 response Effects 0.000 description 2
231100000872 sexual dysfunction Toxicity 0.000 description 2
239000008107 starch Substances 0.000 description 2
235000019698 starch Nutrition 0.000 description 2
230000000638 stimulation Effects 0.000 description 2
239000000725 suspension Substances 0.000 description 2
YAPQBXQYLJRXSA-UHFFFAOYSA-N theobromine Chemical compound CN1C(=O)NC(=O)C2=C1N=CN2C YAPQBXQYLJRXSA-UHFFFAOYSA-N 0.000 description 2
ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 2
210000003462 vein Anatomy 0.000 description 2
GQDDNDAYOVNZPG-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C[C]2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3N=C21 GQDDNDAYOVNZPG-SCYLSFHTSA-N 0.000 description 2
IAPZXUKYTCQQFE-QZKDJMESSA-N (2r,3r,3as,5s)-2-(6-aminopurin-9-yl)-5-[carboxy(hydroxy)methyl]-3-hydroxy-3,3a-dihydro-2h-furo[3,2-b]furan-5-carboxylic acid Chemical class NC1=NC=NC2=C1N=CN2[C@H]1[C@H](O)[C@@H]2O[C@](C(O)=O)(C(O)C(O)=O)C=C2O1 IAPZXUKYTCQQFE-QZKDJMESSA-N 0.000 description 1
125000004169 (C1-C6) alkyl group Chemical group 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
PYHRZPFZZDCOPH-QXGOIDDHSA-N (S)-amphetamine sulfate Chemical compound [H+].[H+].[O-]S([O-])(=O)=O.C[C@H](N)CC1=CC=CC=C1.C[C@H](N)CC1=CC=CC=C1 PYHRZPFZZDCOPH-QXGOIDDHSA-N 0.000 description 1
DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 description 1
RATZLMXRALDSJW-UHFFFAOYSA-N 2-(2-ethyl-3H-benzofuran-2-yl)-4,5-dihydro-1H-imidazole Chemical compound C1C2=CC=CC=C2OC1(CC)C1=NCCN1 RATZLMXRALDSJW-UHFFFAOYSA-N 0.000 description 1
YQAXFVHNHSPUPO-RNJOBUHISA-N 2-[[(2s)-2-[[2-[[(2s,4r)-1-[(2s)-1-(2-aminoacetyl)pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]propanoyl]amino]acetic acid Chemical compound OC(=O)CNC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@H]1N(C(=O)CN)CCC1 YQAXFVHNHSPUPO-RNJOBUHISA-N 0.000 description 1
WJSVJNDMOQTICG-UHFFFAOYSA-N 2-amino-1-[(2-methyl-4-methylidene-5-oxooxolan-2-yl)methyl]-7h-purin-6-one Chemical compound NC1=NC=2N=CNC=2C(=O)N1CC1(C)CC(=C)C(=O)O1 WJSVJNDMOQTICG-UHFFFAOYSA-N 0.000 description 1
FLYJEBSUJDZJDE-UHFFFAOYSA-N 3-phenyl-1h-pyridin-2-one Chemical class O=C1NC=CC=C1C1=CC=CC=C1 FLYJEBSUJDZJDE-UHFFFAOYSA-N 0.000 description 1
HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical class O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 description 1
229930008281 A03AD01 - Papaverine Natural products 0.000 description 1
208000024827 Alzheimer disease Diseases 0.000 description 1
206010002091 Anaesthesia Diseases 0.000 description 1
206010002383 Angina Pectoris Diseases 0.000 description 1
208000019901 Anxiety disease Diseases 0.000 description 1
201000001320 Atherosclerosis Diseases 0.000 description 1
206010004446 Benign prostatic hyperplasia Diseases 0.000 description 1
208000024172 Cardiovascular disease Diseases 0.000 description 1
241000700199 Cavia porcellus Species 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
108090000695 Cytokines Proteins 0.000 description 1
102000004127 Cytokines Human genes 0.000 description 1
208000020401 Depressive disease Diseases 0.000 description 1
239000004097 EU approved flavor enhancer Substances 0.000 description 1
206010016654 Fibrosis Diseases 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
208000010412 Glaucoma Diseases 0.000 description 1
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
108010078321 Guanylate Cyclase Proteins 0.000 description 1
102000014469 Guanylate cyclase Human genes 0.000 description 1
206010019280 Heart failures Diseases 0.000 description 1
239000004705 High-molecular-weight polyethylene Substances 0.000 description 1
206010021118 Hypotonia Diseases 0.000 description 1
206010022076 Injection site infection Diseases 0.000 description 1
LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 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
241000282553 Macaca Species 0.000 description 1
240000003183 Manihot esculenta Species 0.000 description 1
235000016735 Manihot esculenta subsp esculenta Nutrition 0.000 description 1
208000028389 Nerve injury Diseases 0.000 description 1
206010052004 Organic erectile dysfunction Diseases 0.000 description 1
241000283973 Oryctolagus cuniculus Species 0.000 description 1
206010056303 Painful erection Diseases 0.000 description 1
235000019483 Peanut oil Nutrition 0.000 description 1
208000004403 Prostatic Hyperplasia Diseases 0.000 description 1
206010052005 Psychogenic erectile dysfunction Diseases 0.000 description 1
208000006262 Psychological Sexual Dysfunctions Diseases 0.000 description 1
KDCGOANMDULRCW-UHFFFAOYSA-N Purine Natural products N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 description 1
244000000231 Sesamum indicum Species 0.000 description 1
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
244000061456 Solanum tuberosum Species 0.000 description 1
235000002595 Solanum tuberosum Nutrition 0.000 description 1
102000007637 Soluble Guanylyl Cyclase Human genes 0.000 description 1
108010007205 Soluble Guanylyl Cyclase Proteins 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
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 1
208000027418 Wounds and injury Diseases 0.000 description 1
230000002159 abnormal effect Effects 0.000 description 1
230000005856 abnormality Effects 0.000 description 1
239000002253 acid Substances 0.000 description 1
150000007513 acids Chemical class 0.000 description 1
230000004913 activation Effects 0.000 description 1
239000000670 adrenergic alpha-2 receptor antagonist Substances 0.000 description 1
230000002411 adverse Effects 0.000 description 1
102000030619 alpha-1 Adrenergic Receptor Human genes 0.000 description 1
108020004102 alpha-1 Adrenergic Receptor Proteins 0.000 description 1
230000037005 anaesthesia Effects 0.000 description 1
108010082685 antiarrhythmic peptide Proteins 0.000 description 1
230000036506 anxiety Effects 0.000 description 1
210000000709 aorta Anatomy 0.000 description 1
239000012736 aqueous medium Substances 0.000 description 1
239000007900 aqueous suspension Substances 0.000 description 1
210000001367 artery Anatomy 0.000 description 1
238000003556 assay Methods 0.000 description 1
WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
230000003851 biochemical process Effects 0.000 description 1
230000000903 blocking effect Effects 0.000 description 1
230000017531 blood circulation Effects 0.000 description 1
229960001948 caffeine Drugs 0.000 description 1
VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 1
229910000019 calcium carbonate Inorganic materials 0.000 description 1
239000001506 calcium phosphate Substances 0.000 description 1
229910000389 calcium phosphate Inorganic materials 0.000 description 1
235000011010 calcium phosphates Nutrition 0.000 description 1
239000002327 cardiovascular agent Substances 0.000 description 1
229940125692 cardiovascular agent Drugs 0.000 description 1
210000003169 central nervous system Anatomy 0.000 description 1
210000003710 cerebral cortex Anatomy 0.000 description 1
239000003153 chemical reaction reagent Substances 0.000 description 1
230000001684 chronic effect Effects 0.000 description 1
238000003776 cleavage reaction Methods 0.000 description 1
208000010877 cognitive disease Diseases 0.000 description 1
239000003086 colorant Substances 0.000 description 1
239000006071 cream Substances 0.000 description 1
125000004122 cyclic group Chemical group 0.000 description 1
230000006378 damage Effects 0.000 description 1
230000001419 dependent effect Effects 0.000 description 1
AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 description 1
229960003529 diazepam Drugs 0.000 description 1
239000007884 disintegrant Substances 0.000 description 1
239000002934 diuretic Substances 0.000 description 1
229950001765 efaroxan Drugs 0.000 description 1
229920001971 elastomer Polymers 0.000 description 1
230000008030 elimination Effects 0.000 description 1
238000003379 elimination reaction Methods 0.000 description 1
239000003995 emulsifying agent Substances 0.000 description 1
201000003104 endogenous depression Diseases 0.000 description 1
239000003623 enhancer Substances 0.000 description 1
229960005139 epinephrine Drugs 0.000 description 1
238000011156 evaluation Methods 0.000 description 1
230000029142 excretion Effects 0.000 description 1
230000004761 fibrosis Effects 0.000 description 1
239000000945 filler Substances 0.000 description 1
208000017561 flaccidity Diseases 0.000 description 1
235000019264 food flavour enhancer Nutrition 0.000 description 1
235000003599 food sweetener Nutrition 0.000 description 1
238000009472 formulation Methods 0.000 description 1
239000000499 gel Substances 0.000 description 1
239000008273 gelatin Substances 0.000 description 1
229920000159 gelatin Polymers 0.000 description 1
239000007903 gelatin capsule Substances 0.000 description 1
235000019322 gelatine Nutrition 0.000 description 1
235000011852 gelatine desserts Nutrition 0.000 description 1
239000008103 glucose Substances 0.000 description 1
150000004677 hydrates Chemical class 0.000 description 1
HOFSPGAYXKNFAM-UHFFFAOYSA-N imidazo[4,5-f]quinoxalin-2-one Chemical class C1=CN=C2C3=NC(=O)N=C3C=CC2=N1 HOFSPGAYXKNFAM-UHFFFAOYSA-N 0.000 description 1
230000006872 improvement Effects 0.000 description 1
238000000099 in vitro assay Methods 0.000 description 1
238000001727 in vivo Methods 0.000 description 1
230000002401 inhibitory effect Effects 0.000 description 1
230000005764 inhibitory process Effects 0.000 description 1
208000014674 injury Diseases 0.000 description 1
238000007918 intramuscular administration Methods 0.000 description 1
239000007927 intramuscular injection Substances 0.000 description 1
239000007928 intraperitoneal injection Substances 0.000 description 1
238000001990 intravenous administration Methods 0.000 description 1
VCMGMSHEPQENPE-UHFFFAOYSA-N ketamine hydrochloride Chemical compound [Cl-].C=1C=CC=C(Cl)C=1C1([NH2+]C)CCCCC1=O VCMGMSHEPQENPE-UHFFFAOYSA-N 0.000 description 1
239000008101 lactose Substances 0.000 description 1
210000005246 left atrium Anatomy 0.000 description 1
230000004130 lipolysis Effects 0.000 description 1
239000007788 liquid Substances 0.000 description 1
239000006210 lotion Substances 0.000 description 1
229940083747 low-ceiling diuretics xanthine derivative Drugs 0.000 description 1
239000007937 lozenge Substances 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
235000019359 magnesium stearate Nutrition 0.000 description 1
208000024714 major depressive disease Diseases 0.000 description 1
206010027175 memory impairment Diseases 0.000 description 1
230000004060 metabolic process Effects 0.000 description 1
239000002207 metabolite Substances 0.000 description 1
MXELDPKESKXREN-UHFFFAOYSA-N methyl 5-[3-(4,4-diphenylpiperidin-1-yl)propylcarbamoyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carboxylate;hydrochloride Chemical compound Cl.COC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(CC2)(C=2C=CC=CC=2)C=2C=CC=CC=2)C1C1=CC=C([N+]([O-])=O)C=C1 MXELDPKESKXREN-UHFFFAOYSA-N 0.000 description 1
239000000472 muscarinic agonist Substances 0.000 description 1
210000003205 muscle Anatomy 0.000 description 1
229960005016 naphazoline Drugs 0.000 description 1
230000001452 natriuretic effect Effects 0.000 description 1
210000005036 nerve Anatomy 0.000 description 1
230000008764 nerve damage Effects 0.000 description 1
210000001640 nerve ending Anatomy 0.000 description 1
208000015122 neurodegenerative disease Diseases 0.000 description 1
201000001119 neuropathy Diseases 0.000 description 1
230000007823 neuropathy Effects 0.000 description 1
230000003957 neurotransmitter release Effects 0.000 description 1
239000002674 ointment Substances 0.000 description 1
239000006186 oral dosage form Substances 0.000 description 1
210000000056 organ Anatomy 0.000 description 1
238000012858 packaging process Methods 0.000 description 1
229960001789 papaverine Drugs 0.000 description 1
230000001734 parasympathetic effect Effects 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
239000003182 parenteral nutrition solution Substances 0.000 description 1
239000000312 peanut oil Substances 0.000 description 1
230000002093 peripheral effect Effects 0.000 description 1
210000001428 peripheral nervous system Anatomy 0.000 description 1
208000033808 peripheral neuropathy Diseases 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
230000035790 physiological processes and functions Effects 0.000 description 1
239000002504 physiological saline solution Substances 0.000 description 1
239000004033 plastic Substances 0.000 description 1
125000003367 polycyclic group Chemical group 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
239000000843 powder Substances 0.000 description 1
WFXFYZULCQKPIP-UHFFFAOYSA-N prazosin hydrochloride Chemical compound [H+].[Cl-].N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(CC1)CCN1C(=O)C1=CC=CO1 WFXFYZULCQKPIP-UHFFFAOYSA-N 0.000 description 1
229960002386 prazosin hydrochloride Drugs 0.000 description 1
239000000651 prodrug Substances 0.000 description 1
229940002612 prodrug Drugs 0.000 description 1
230000002035 prolonged effect Effects 0.000 description 1
102000004169 proteins and genes Human genes 0.000 description 1
108090000623 proteins and genes Proteins 0.000 description 1
208000020016 psychiatric disease Diseases 0.000 description 1
150000008518 pyridopyrimidines Chemical class 0.000 description 1
DRYRBWIFRVMRPV-UHFFFAOYSA-N quinazolin-4-amine Chemical class C1=CC=C2C(N)=NC=NC2=C1 DRYRBWIFRVMRPV-UHFFFAOYSA-N 0.000 description 1
125000001567 quinoxalinyl group Chemical class N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
239000011347 resin Substances 0.000 description 1
229920005989 resin Polymers 0.000 description 1
HJORMJIFDVBMOB-UHFFFAOYSA-N rolipram Chemical compound COC1=CC=C(C2CC(=O)NC2)C=C1OC1CCCC1 HJORMJIFDVBMOB-UHFFFAOYSA-N 0.000 description 1
229950005741 rolipram Drugs 0.000 description 1
238000007665 sagging Methods 0.000 description 1
230000007017 scission Effects 0.000 description 1
239000008159 sesame oil Substances 0.000 description 1
235000011803 sesame oil Nutrition 0.000 description 1
150000004760 silicates Chemical class 0.000 description 1
210000002460 smooth muscle Anatomy 0.000 description 1
230000016160 smooth muscle contraction Effects 0.000 description 1
210000000329 smooth muscle myocyte Anatomy 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
239000001509 sodium citrate Substances 0.000 description 1
NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
235000019333 sodium laurylsulphate Nutrition 0.000 description 1
230000000392 somatic effect Effects 0.000 description 1
208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
238000012289 standard assay Methods 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
238000007920 subcutaneous administration Methods 0.000 description 1
239000007929 subcutaneous injection Substances 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
238000001356 surgical procedure Methods 0.000 description 1
239000000375 suspending agent Substances 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
230000002889 sympathetic effect Effects 0.000 description 1
210000002820 sympathetic nervous system Anatomy 0.000 description 1
208000024891 symptom Diseases 0.000 description 1
WOXKDUGGOYFFRN-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 WOXKDUGGOYFFRN-IIBYNOLFSA-N 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
229960001909 terazosin hydrochloride Drugs 0.000 description 1
IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 description 1
229960004559 theobromine Drugs 0.000 description 1
229960000278 theophylline Drugs 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
238000011200 topical administration Methods 0.000 description 1
230000000699 topical effect Effects 0.000 description 1
239000006211 transdermal dosage form Substances 0.000 description 1
QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
210000001215 vagina Anatomy 0.000 description 1
239000003981 vehicle Substances 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
238000005303 weighing Methods 0.000 description 1
REZGGXNDEMKIQB-UHFFFAOYSA-N zaprinast Chemical compound CCCOC1=CC=CC=C1C1=NC(=O)C2=NNNC2=N1 REZGGXNDEMKIQB-UHFFFAOYSA-N 0.000 description 1
229950005371 zaprinast 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
- 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- 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
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
- 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
- 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
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
- 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)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Reproductive Health (AREA)
Endocrinology (AREA)
Gynecology & Obstetrics (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Medicines Containing Plant Substances (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

SK878-2000A 1997-12-16 1998-10-29 Combination, composition and kits effective for the treatment of impotence SK8782000A3 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US6974197P	1997-12-16	1997-12-16
PCT/IB1998/001723 WO1999030697A2 (en)	1997-12-16	1998-10-29	Combination effective for the treatment of impotence

Publications (1)

Publication Number	Publication Date
SK8782000A3 true SK8782000A3 (en)	2002-03-05

Family

ID=22090927

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK878-2000A SK8782000A3 (en)	1997-12-16	1998-10-29	Combination, composition and kits effective for the treatment of impotence

Country Status (37)

Country	Link
EP (1)	EP1037616B1 (cs)
JP (2)	JP2002508315A (cs)
KR (1)	KR20010033092A (cs)
CN (1)	CN1282248A (cs)
AP (1)	AP915A (cs)
AR (1)	AR016433A1 (cs)
AT (1)	ATE318602T1 (cs)
AU (1)	AU759825B2 (cs)
BG (1)	BG104528A (cs)
BR (1)	BR9813699A (cs)
CA (1)	CA2314993A1 (cs)
CO (1)	CO4810381A1 (cs)
CZ (1)	CZ20002199A3 (cs)
DE (1)	DE69833671T2 (cs)
DZ (1)	DZ2675A1 (cs)
EA (1)	EA200000526A1 (cs)
ES (1)	ES2258300T3 (cs)
GT (1)	GT199800177A (cs)
HN (1)	HN1998000174A (cs)
HR (1)	HRP20000407A2 (cs)
HU (1)	HUP0100705A3 (cs)
IL (1)	IL136515A0 (cs)
IS (1)	IS5504A (cs)
MA (1)	MA26586A1 (cs)
NO (1)	NO20003065L (cs)
NZ (1)	NZ504487A (cs)
OA (1)	OA11423A (cs)
PA (1)	PA8462801A1 (cs)
PE (1)	PE20000011A1 (cs)
PL (1)	PL341575A1 (cs)
SK (1)	SK8782000A3 (cs)
TN (1)	TNSN98227A1 (cs)
TR (1)	TR200001733T2 (cs)
UY (1)	UY25300A1 (cs)
WO (1)	WO1999030697A2 (cs)
YU (1)	YU33700A (cs)
ZA (1)	ZA9811507B (cs)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6469065B1 (en)	1996-02-02	2002-10-22	Nitromed, Inc.	Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
US6331543B1 (en)	1996-11-01	2001-12-18	Nitromed, Inc.	Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
DE19844162A1 (de) *	1998-09-25	2000-03-30	Udo Dunzendorfer	Medikamentenkombinationen zur Therapie der erektilen Dysfunktion
AU3724400A (en) *	1999-03-08	2000-09-28	Merck & Co., Inc.	Methods and compositions for treating erectile dysfunction
US7235625B2 (en) *	1999-06-29	2007-06-26	Palatin Technologies, Inc.	Multiple agent therapy for sexual dysfunction
ATE399554T1 (de) *	1999-08-03	2008-07-15	Lilly Icos Llc	Pharmazeutische zusammensetzung enthaltend tadalafil
TWI265925B (en)	1999-10-11	2006-11-11	Pfizer	Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them
AU2000270300A1 (en) *	2000-09-13	2002-03-26	Isis Innovation Limited	Use of phosphodiesterase inhibitors for the treatment of anorectal disorders
EP1333824B1 (en) *	2000-11-17	2005-09-07	Warner-Lambert Company LLC	Treatment of sexual dysfunction with bombesin receptor antagonists
US20030114469A1 (en) *	2001-09-27	2003-06-19	Cohen David Saul	Combinations
GB0219961D0 (en)	2002-08-28	2002-10-02	Pfizer Ltd	Oxytocin inhibitors
GB0225908D0 (en) *	2002-11-06	2002-12-11	Pfizer Ltd	Treatment of female sexual dysfunction
US7323462B2 (en)	2002-12-10	2008-01-29	Pfizer Inc.	Morpholine dopamine agonists
CA2451267A1 (en)	2002-12-13	2004-06-13	Warner-Lambert Company Llc	Pharmaceutical uses for alpha2delta ligands
US7291640B2 (en)	2003-09-22	2007-11-06	Pfizer Inc.	Substituted triazole derivatives as oxytocin antagonists
AP2007004047A0 (en)	2005-01-20	2007-06-30	Pfizer Ltd	Substituted triazole derivatives as oxtocin antagonists
US8506934B2 (en)	2005-04-29	2013-08-13	Robert I. Henkin	Methods for detection of biological substances
US8067433B2 (en)	2005-11-09	2011-11-29	Zalicus Inc.	Methods, compositions, and kits for the treatment of ophthalmic disorders
WO2008095136A2 (en)	2007-01-31	2008-08-07	Henkin Robert I	Methods for detection of biological substances
US8580801B2 (en)	2008-07-23	2013-11-12	Robert I. Henkin	Phosphodiesterase inhibitor treatment
CN101781302B (zh) *	2009-05-31	2013-07-10	段波	一种磷酸二酯酶抑制剂和异黄酮形成的加成物及其应用
WO2013106547A1 (en)	2012-01-10	2013-07-18	President And Fellows Of Harvard College	Beta-cell replication promoting compounds and methods of their use
WO2014055801A1 (en)	2012-10-05	2014-04-10	Henkin Robert I	Phosphodiesterase inhibitors for treating taste and smell disorders
WO2015126944A1 (en)	2014-02-18	2015-08-27	Henkin Robert I	Methods and compositions for diagnosing and treating loss and/or distortion of taste or smell
US11590209B2 (en)	2020-01-21	2023-02-28	Palatin Technologies, Inc.	Use of bremelanotide in patients with controlled hypertension
CN115485027A (zh)	2020-03-24	2022-12-16	思瑞诺医疗有限公司	冠状病毒感染引起的化学感觉功能障碍的治疗

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ZA878182B (en) *	1986-11-05	1988-05-02	Merrell Dow Pharmaceuticals Inc.	Enhancement of prazosin
FR2649613B1 (fr) *	1989-07-11	1991-09-27	Virag Ronald	Medicament vaso-actif
US5242391A (en) *	1990-04-25	1993-09-07	Alza Corporation	Urethral insert for treatment of erectile dysfunction
DK0459666T3 (da) *	1990-05-31	1994-12-05	Pfizer	Lægemidler mod impotens
GB9301192D0 (en) *	1993-06-09	1993-06-09	Trott Francis W	Flower shaped mechanised table
GB9523752D0 (en) *	1995-11-21	1996-01-24	Pfizer Ltd	Pharmaceutical formulations

1998
- 1998-10-29 BR BR9813699-2A patent/BR9813699A/pt not_active Application Discontinuation
- 1998-10-29 NZ NZ504487A patent/NZ504487A/xx unknown
- 1998-10-29 DE DE69833671T patent/DE69833671T2/de not_active Expired - Fee Related
- 1998-10-29 EP EP98947741A patent/EP1037616B1/en not_active Revoked
- 1998-10-29 CN CN98812331A patent/CN1282248A/zh active Pending
- 1998-10-29 KR KR1020007006455A patent/KR20010033092A/ko not_active Ceased
- 1998-10-29 CA CA002314993A patent/CA2314993A1/en not_active Abandoned
- 1998-10-29 YU YU33700A patent/YU33700A/sh unknown
- 1998-10-29 HU HU0100705A patent/HUP0100705A3/hu unknown
- 1998-10-29 TR TR2000/01733T patent/TR200001733T2/xx unknown
- 1998-10-29 HR HR20000407A patent/HRP20000407A2/hr not_active Application Discontinuation
- 1998-10-29 IL IL13651598A patent/IL136515A0/xx unknown
- 1998-10-29 SK SK878-2000A patent/SK8782000A3/sk unknown
- 1998-10-29 AT AT98947741T patent/ATE318602T1/de not_active IP Right Cessation
- 1998-10-29 AU AU94558/98A patent/AU759825B2/en not_active Ceased
- 1998-10-29 CZ CZ20002199A patent/CZ20002199A3/cs unknown
- 1998-10-29 JP JP2000538680A patent/JP2002508315A/ja active Pending
- 1998-10-29 EA EA200000526A patent/EA200000526A1/ru unknown
- 1998-10-29 ES ES98947741T patent/ES2258300T3/es not_active Expired - Lifetime
- 1998-10-29 WO PCT/IB1998/001723 patent/WO1999030697A2/en not_active Ceased
- 1998-10-29 PL PL98341575A patent/PL341575A1/xx unknown
- 1998-11-09 GT GT199800177A patent/GT199800177A/es unknown
- 1998-11-10 PA PA19988462801A patent/PA8462801A1/es unknown
- 1998-11-11 HN HN1998000174A patent/HN1998000174A/es unknown
- 1998-11-30 CO CO98070722A patent/CO4810381A1/es unknown
- 1998-12-10 AP APAP/P/1998/001414A patent/AP915A/en active
- 1998-12-11 PE PE1998001206A patent/PE20000011A1/es not_active Application Discontinuation
- 1998-12-14 UY UY25300A patent/UY25300A1/es not_active Application Discontinuation
- 1998-12-15 MA MA25396A patent/MA26586A1/fr unknown
- 1998-12-15 AR ARP980106360A patent/AR016433A1/es unknown
- 1998-12-15 TN TNTNSN98227A patent/TNSN98227A1/fr unknown
- 1998-12-15 DZ DZ980285A patent/DZ2675A1/xx active
- 1998-12-15 ZA ZA9811507A patent/ZA9811507B/xx unknown
2000
- 2000-05-19 IS IS5504A patent/IS5504A/is unknown
- 2000-06-13 BG BG104528A patent/BG104528A/xx unknown
- 2000-06-15 OA OA1200000169A patent/OA11423A/en unknown
- 2000-06-15 NO NO20003065A patent/NO20003065L/no not_active Application Discontinuation
2007
- 2007-08-20 JP JP2007213745A patent/JP2007332156A/ja not_active Withdrawn

Also Published As

Publication number	Publication date
AP9801414A0 (en)	1998-12-31
GT199800177A (es)	2000-05-02
CN1282248A (zh)	2001-01-31
BG104528A (en)	2001-02-28
CA2314993A1 (en)	1999-06-24
DE69833671T2 (de)	2006-11-30
TR200001733T2 (tr)	2000-11-21
HRP20000407A2 (en)	2000-10-31
JP2007332156A (ja)	2007-12-27
NZ504487A (en)	2002-11-26
ES2258300T3 (es)	2006-08-16
IL136515A0 (en)	2001-06-14
EA200000526A1 (ru)	2000-12-25
KR20010033092A (ko)	2001-04-25
AU9455898A (en)	1999-07-05
CO4810381A1 (es)	1999-06-30
NO20003065D0 (no)	2000-06-15
PA8462801A1 (es)	2000-05-24
YU33700A (sh)	2004-05-12
HN1998000174A (es)	1999-01-08
EP1037616A2 (en)	2000-09-27
HUP0100705A2 (hu)	2001-08-28
WO1999030697A2 (en)	1999-06-24
WO1999030697A3 (en)	1999-08-26
IS5504A (is)	2000-05-19
ZA9811507B (en)	2000-06-19
TNSN98227A1 (fr)	2005-03-15
AU759825B2 (en)	2003-05-01
AR016433A1 (es)	2001-07-04
DZ2675A1 (fr)	2003-03-29
PE20000011A1 (es)	2000-01-18
UY25300A1 (es)	2000-12-29
ATE318602T1 (de)	2006-03-15
EP1037616B1 (en)	2006-03-01
JP2002508315A (ja)	2002-03-19
HUP0100705A3 (en)	2001-12-28
NO20003065L (no)	2000-08-15
AP915A (en)	2000-12-18
BR9813699A (pt)	2000-10-10
OA11423A (en)	2004-04-21
PL341575A1 (en)	2001-04-23
MA26586A1 (fr)	2004-12-20
DE69833671D1 (de)	2006-04-27
CZ20002199A3 (cs)	2001-10-17

Publication	Publication Date	Title
EP1037616B1 (en)	2006-03-01	COMBINATION OF ALPHA-1-ADRENERGIC ANTAGONISTS AND A CGMP PDEv INHIBITOR FOR THE TREATMENT OF IMPOTENCE
US6127363A (en)	2000-10-03	Local administration of Type IV phosphodiesterase inhibitors for the treatment of erectile dysfunction
US6156753A (en)	2000-12-05	Local administration of type III phosphodiesterase inhibitors for the treatment of erectile dysfunction
JP6247249B2 (ja)	2017-12-13	眼障害のためのｐｄｅ１阻害剤
US6037346A (en)	2000-03-14	Local administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
AU2009324495B2 (en)	2015-12-24	Methods for treating multiple sclerosis using tetracyclic pyrazinoindoles
EP1020190A2 (en)	2000-07-19	Treatment of BPH with cGMP elevators
US6476037B1 (en)	2002-11-05	L-arginine and phosphodiesterase (PDE) inhibitor synergism
US20020004498A1 (en)	2002-01-10	Transmucosal administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
KR20010089779A (ko)	2001-10-08	성적 장애의 치료 방법
AU1112901A (en)	2001-07-19	Compositions and methods of treatment for conditions responsive to testosterone elevation
WO1999021558A2 (en)	1999-05-06	Local administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
US6436944B1 (en)	2002-08-20	Combination effective for the treatment of impotence
US20020147199A1 (en)	2002-10-10	Process for the treatment of erectile dysfunction and product therefor
US20060142282A1 (en)	2006-06-29	Combination effective for the treatment of impotence
HK1032911A (en)	2001-08-10	Combination effective for the treatment of impotence
MXPA00009614A (en)	2002-05-09	Combination effective for the treatment of impotence comprising a potassium-channel-opener and a cgmp elevator
JP2002249446A (ja)	2002-09-06	不能の治療に効果的な多剤併用薬
AU2005248938A1 (en)	2006-02-02	Transmucosal composition containing a phosphodiesterase inhibitor for the treatment of erectile dysfunction