AR040090A1 - NEW COMBINATION - Google Patents
NEW COMBINATIONInfo
- Publication number
- AR040090A1 AR040090A1 ARP030101762A ARP030101762A AR040090A1 AR 040090 A1 AR040090 A1 AR 040090A1 AR P030101762 A ARP030101762 A AR P030101762A AR P030101762 A ARP030101762 A AR P030101762A AR 040090 A1 AR040090 A1 AR 040090A1
- Authority
- AR
- Argentina
- Prior art keywords
- sildenafil citrate
- hypertension
- methyl
- inhibitor
- sildenafil
- Prior art date
Links
- DEIYFTQMQPDXOT-UHFFFAOYSA-N sildenafil citrate Chemical group 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 abstract 9
- 229960002639 sildenafil citrate Drugs 0.000 abstract 9
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical group 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 abstract 6
- 206010020772 Hypertension Diseases 0.000 abstract 3
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 abstract 3
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- BIDNLKIUORFRQP-XYGFDPSESA-N (2s,4s)-4-cyclohexyl-1-[2-[[(1s)-2-methyl-1-propanoyloxypropoxy]-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid Chemical compound C([P@@](=O)(O[C@H](OC(=O)CC)C(C)C)CC(=O)N1[C@@H](C[C@H](C1)C1CCCCC1)C(O)=O)CCCC1=CC=CC=C1 BIDNLKIUORFRQP-XYGFDPSESA-N 0.000 abstract 2
- -1 3,4-Methylenedioxyphenyl Chemical group 0.000 abstract 2
- 239000005541 ACE inhibitor Substances 0.000 abstract 2
- 108010061435 Enalapril Proteins 0.000 abstract 2
- 108010007859 Lisinopril Proteins 0.000 abstract 2
- VXFJYXUZANRPDJ-WTNASJBWSA-N Trandopril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@H]2CCCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 VXFJYXUZANRPDJ-WTNASJBWSA-N 0.000 abstract 2
- 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 abstract 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 abstract 2
- 229960000830 captopril Drugs 0.000 abstract 2
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 abstract 2
- 206010012601 diabetes mellitus Diseases 0.000 abstract 2
- 229960000873 enalapril Drugs 0.000 abstract 2
- GBXSMTUPTTWBMN-XIRDDKMYSA-N enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 abstract 2
- 229960002490 fosinopril Drugs 0.000 abstract 2
- 229960002394 lisinopril Drugs 0.000 abstract 2
- RLAWWYSOJDYHDC-BZSNNMDCSA-N lisinopril Chemical compound C([C@H](N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(O)=O)C(O)=O)CC1=CC=CC=C1 RLAWWYSOJDYHDC-BZSNNMDCSA-N 0.000 abstract 2
- 229960003401 ramipril Drugs 0.000 abstract 2
- HDACQVRGBOVJII-JBDAPHQKSA-N ramipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@@H]2CCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 HDACQVRGBOVJII-JBDAPHQKSA-N 0.000 abstract 2
- 229960003310 sildenafil Drugs 0.000 abstract 2
- 229960002051 trandolapril Drugs 0.000 abstract 2
- INLBUQIADGPECI-UHFFFAOYSA-N 5-(5-acetyl-2-butoxypyridin-3-yl)-3-ethyl-2-(1-ethylazetidin-3-yl)-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound CCCCOC1=NC=C(C(C)=O)C=C1C1=NC2=C(CC)N(C3CN(CC)C3)N=C2C(=O)N1 INLBUQIADGPECI-UHFFFAOYSA-N 0.000 abstract 1
- YPFZMBHKIVDSNR-UHFFFAOYSA-N 5-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylpyridin-3-yl]-3-ethyl-2-(2-methoxyethyl)-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound C1=C(C=2NC(=O)C3=NN(CCOC)C(CC)=C3N=2)C(OCC)=NC=C1S(=O)(=O)N1CCN(CC)CC1 YPFZMBHKIVDSNR-UHFFFAOYSA-N 0.000 abstract 1
- FFCZQVKVWGGQFB-UHFFFAOYSA-N 9h-pyrido[3,4-b]indole-1,4-dione Chemical compound N1C2=CC=CC=C2C2=C1C(=O)N=CC2=O FFCZQVKVWGGQFB-UHFFFAOYSA-N 0.000 abstract 1
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 102000015427 Angiotensins Human genes 0.000 abstract 1
- 108010064733 Angiotensins Proteins 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- XPCFTKFZXHTYIP-PMACEKPBSA-N Benazepril Chemical group C([C@@H](C(=O)OCC)N[C@@H]1C(N(CC(O)=O)C2=CC=CC=C2CC1)=O)CC1=CC=CC=C1 XPCFTKFZXHTYIP-PMACEKPBSA-N 0.000 abstract 1
- 206010007559 Cardiac failure congestive Diseases 0.000 abstract 1
- 101100189582 Dictyostelium discoideum pdeD gene Proteins 0.000 abstract 1
- 108010066671 Enalaprilat Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 208000007530 Essential hypertension Diseases 0.000 abstract 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 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- UWWDHYUMIORJTA-HSQYWUDLSA-N Moexipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC(OC)=C(OC)C=C2C1)C(O)=O)CC1=CC=CC=C1 UWWDHYUMIORJTA-HSQYWUDLSA-N 0.000 abstract 1
- 101150098694 PDE5A gene Proteins 0.000 abstract 1
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 abstract 1
- 201000003099 Renovascular Hypertension Diseases 0.000 abstract 1
- 201000004239 Secondary hypertension Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 206010042957 Systolic hypertension Diseases 0.000 abstract 1
- 230000004075 alteration Effects 0.000 abstract 1
- 229960004530 benazepril Drugs 0.000 abstract 1
- 229960003619 benazepril hydrochloride Drugs 0.000 abstract 1
- VPSRQEHTHIMDQM-FKLPMGAJSA-N benazepril hydrochloride Chemical compound Cl.C([C@@H](C(=O)OCC)N[C@@H]1C(N(CC(O)=O)C2=CC=CC=C2CC1)=O)CC1=CC=CC=C1 VPSRQEHTHIMDQM-FKLPMGAJSA-N 0.000 abstract 1
- 102100029175 cGMP-specific 3',5'-cyclic phosphodiesterase Human genes 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 238000009109 curative therapy Methods 0.000 abstract 1
- ZOOGRGPOEVQQDX-KHLHZJAASA-N cyclic guanosine monophosphate Chemical compound C([C@H]1O2)O[P@](O)(=O)O[C@@H]1[C@H](O)[C@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-KHLHZJAASA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229960002680 enalaprilat Drugs 0.000 abstract 1
- LZFZMUMEGBBDTC-QEJZJMRPSA-N enalaprilat (anhydrous) Chemical compound C([C@H](N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)C(O)=O)CC1=CC=CC=C1 LZFZMUMEGBBDTC-QEJZJMRPSA-N 0.000 abstract 1
- 239000008103 glucose Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 abstract 1
- 229960005170 moexipril Drugs 0.000 abstract 1
- 238000002638 palliative care Methods 0.000 abstract 1
- 229960002582 perindopril Drugs 0.000 abstract 1
- IPVQLZZIHOAWMC-QXKUPLGCSA-N perindopril Chemical compound C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H]21 IPVQLZZIHOAWMC-QXKUPLGCSA-N 0.000 abstract 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000002815 pulmonary hypertension Diseases 0.000 abstract 1
- 229960001455 quinapril Drugs 0.000 abstract 1
- JSDRRTOADPPCHY-HSQYWUDLSA-N quinapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC=CC=C2C1)C(O)=O)CC1=CC=CC=C1 JSDRRTOADPPCHY-HSQYWUDLSA-N 0.000 abstract 1
- 229960003042 quinapril hydrochloride Drugs 0.000 abstract 1
- IBBLRJGOOANPTQ-JKVLGAQCSA-N quinapril hydrochloride Chemical compound Cl.C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC=CC=C2C1)C(O)=O)CC1=CC=CC=C1 IBBLRJGOOANPTQ-JKVLGAQCSA-N 0.000 abstract 1
- 229960000835 tadalafil Drugs 0.000 abstract 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 abstract 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 1
- 229960002381 vardenafil Drugs 0.000 abstract 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
- A61K31/535—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
- A61K31/33—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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Reivindicación 1: El uso de una combinación de un inhibidor de fosfodiesterasa de tipo 5 (PDE5) específica de monofosfato de guanosina cíclico y un inhibidor de la enzima de conversión de la angiotensina (ACE) para la preparación de un medicamento caracterizado porque es para el tratamiento paliativo, curativo o profiláctico de la hipertensión, incluyendo hipertensión esencial, hipertensión pulmonar, hipertensión secundaria, hipertensión sistólica aislada, hipertensión asociada a diabetes, hipertensión asociada a aterosclerosis e hipertensión renovascular, insuficiencia cardíaca congestiva, angina, apoplejía, diabetes y alteración de la tolerancia a la glucosa. Reivindicación 4: El uso según cualquiera de las reivindicaciones precedentes, caracterizado porque el inhibidor de PDE5 se selecciona de 5-[2-etoxi-5-(4-metil-1-piperazinilsulfonil)fenil]-1-metil-3-n-propil-1,6-dihidro-7H-pirazolo[4,3-d]pirimidin-7-ona (sildenafilo) (6R,12aR)-2,3,6,7,12,12a-hexahidro-2-metil-6-(3,4-metilendioxifenil)-pirazino[2',1':6,1]pirido[3,4-b]indol-1,4-diona (tadalafilo); 2-[2-etoxi-5-(4-etilpiperazin-1-il-1-sulfonil)fenil]-5-metil-7-propil-3H-imidazo[5,1-f][1,2,4]triazin-4-ona (vardenafilo); 5-[2-etoxi-5-(4-etilpiperazin-1-ilsulfonil)piridin-3-il]-3-etil-2-[2-metoxietil]-2,6-dihidro-7H-pirazolo[4,3-d]pirimidin-7-ona; y 5-[5-acetil-2-butoxi-3-piridinil)-3-etil-2-(1-etil-3-azetidinil)-2,6-dihidro-7H-pirazolo[4,3-d]pirimidin-7-ona; y las sales farmacéuticamente aceptables de las mismas. Reivindicación 5: El uso según la reivindicación 4, caracterizado porque el inhibidor de PDE5 es 5-[2-etoxi-5-(4-metil-1-piperazinilsulfonil)fenil]-1-metil-3-n-propil-1,6-dihidro-7H-pirazolo[4,3-d]pirimidin-7-ona (sildenafilo) o una sal farmacéuticamente aceptable de la misma. Reivindicación 7: El uso según cualquiera de las reivindicaciones precedentes, caracterizado porque el inhibidor de ACE se selecciona de benazepril, captopril, cilazepril, enalapril, enalaprilat, fosinopril, lisinopril, moexepril, perindopril, quinapril, ramipril y trandolapril y las sales farmacéuticamente aceptables de los mismos. Reivindicación 8: El uso según la reivindicación 7, caracterizado porque la combinación del inhibidor de PDE5 y el inhibidor de ACE se selecciona de citrato de sildenafilo y clorhidrato de quinapril; citrato de sildenafilo y clorhidrato de benazepril; citrato de sildenafilo y captopril; citrato de sildenafilo y maleato de enalapril; citrato de sildenafilo y fosinopril; citrato de sildenafilo y lisinopril; citrato de sildenafilo y moexipril; citrato de sildenafilo y ramipril; citrato de sildenafilo y trandolapril.Claim 1: The use of a combination of a cyclic guanosine monophosphate type 5 (PDE5) phosphodiesterase inhibitor and an angiotensin conversion enzyme (ACE) inhibitor for the preparation of a medicament characterized in that it is for the Palliative, curative or prophylactic treatment of hypertension, including essential hypertension, pulmonary hypertension, secondary hypertension, isolated systolic hypertension, hypertension associated with diabetes, hypertension associated with atherosclerosis and renovascular hypertension, congestive heart failure, angina, stroke, diabetes and alteration of the glucose tolerance Claim 4: The use according to any of the preceding claims, characterized in that the PDE5 inhibitor is selected from 5- [2-ethoxy-5- (4-methyl-1-piperazinylsulfonyl) phenyl] -1-methyl-3-n- propyl-1,6-dihydro-7H-pyrazolo [4,3-d] pyrimidin-7-one (sildenafil) (6R, 12aR) -2,3,6,7,12,12a-hexahydro-2-methyl- 6- (3,4-Methylenedioxyphenyl) -pyrazino [2 ', 1': 6.1] pyrido [3,4-b] indole-1,4-dione (tadalafil); 2- [2-Ethoxy-5- (4-ethylpiperazin-1-yl-1-sulfonyl) phenyl] -5-methyl-7-propyl-3H-imidazo [5,1-f] [1,2,4] triazin-4-one (vardenafil); 5- [2-Ethoxy-5- (4-ethylpiperazin-1-ylsulfonyl) pyridin-3-yl] -3-ethyl-2- [2-methoxyethyl] -2,6-dihydro-7H-pyrazolo [4,3 -d] pyrimidin-7-one; and 5- [5-acetyl-2-butoxy-3-pyridinyl) -3-ethyl-2- (1-ethyl-3-azetidinyl) -2,6-dihydro-7H-pyrazolo [4,3-d] pyrimidin -7-one; and pharmaceutically acceptable salts thereof. Claim 5: The use according to claim 4, characterized in that the PDE5 inhibitor is 5- [2-ethoxy-5- (4-methyl-1-piperazinylsulfonyl) phenyl] -1-methyl-3-n-propyl-1, 6-dihydro-7H-pyrazolo [4,3-d] pyrimidin-7-one (sildenafil) or a pharmaceutically acceptable salt thereof. Claim 7: The use according to any of the preceding claims, characterized in that the ACE inhibitor is selected from benazepril, captopril, cilazepril, enalapril, enalaprilat, fosinopril, lisinopril, moexepril, perindopril, quinapril, ramipril and trandolapril and the pharmaceutically acceptable salts of the same. Claim 8: The use according to claim 7, characterized in that the combination of the PDE5 inhibitor and the ACE inhibitor is selected from sildenafil citrate and quinapril hydrochloride; sildenafil citrate and benazepril hydrochloride; sildenafil citrate and captopril; Enalapril Sildenafil Citrate and Maleate; sildenafil citrate and fosinopril; sildenafil citrate and lisinopril; sildenafil citrate and moexipril; sildenafil citrate and ramipril; Sildenafil Citrate and Trandolapril.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0211919A GB0211919D0 (en) | 2002-05-23 | 2002-05-23 | Novel combination |
| GB0229784A GB0229784D0 (en) | 2002-12-20 | 2002-12-20 | Novel combination |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040090A1 true AR040090A1 (en) | 2005-03-16 |
Family
ID=29585817
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030101762A AR040090A1 (en) | 2002-05-23 | 2003-05-21 | NEW COMBINATION |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP1506015A2 (en) |
| JP (1) | JP2005529927A (en) |
| KR (1) | KR20050004195A (en) |
| CN (1) | CN1655820A (en) |
| AR (1) | AR040090A1 (en) |
| AU (1) | AU2003223071A1 (en) |
| BR (1) | BR0311191A (en) |
| CA (1) | CA2485984A1 (en) |
| IL (1) | IL164975A0 (en) |
| MX (1) | MXPA04010951A (en) |
| NO (1) | NO20045517L (en) |
| PA (1) | PA8574201A1 (en) |
| PE (1) | PE20040514A1 (en) |
| PL (1) | PL374198A1 (en) |
| RU (1) | RU2004133973A (en) |
| TW (1) | TW200407153A (en) |
| UY (1) | UY27816A1 (en) |
| WO (1) | WO2003099194A2 (en) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7019010B2 (en) | 2001-09-27 | 2006-03-28 | Novertis Ag | Combinations |
| GB0318094D0 (en) * | 2003-08-01 | 2003-09-03 | Pfizer Ltd | Novel combination |
| DE102004011512B4 (en) | 2004-03-08 | 2022-01-13 | Boehringer Ingelheim Vetmedica Gmbh | Pharmaceutical preparation containing pimobendan |
| US8980894B2 (en) | 2004-03-25 | 2015-03-17 | Boehringer Ingelheim Vetmedica Gmbh | Use of PDE III inhibitors for the treatment of asymptomatic (occult) heart failure |
| EP1579862A1 (en) * | 2004-03-25 | 2005-09-28 | Boehringer Ingelheim Vetmedica Gmbh | Use of PDE III inhibitors for the reduction of heart size in mammals suffering from heart failure |
| FR2902009B1 (en) * | 2006-06-13 | 2012-12-07 | Bioprojet Soc Civ | USE OF A VASOPEPTIDASE INHIBITOR FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION |
| BRPI0716571A2 (en) * | 2006-08-24 | 2013-11-05 | Surface Logix Inc | PHARMACEUTICALLY OPTIMIZED COMPOUNDS |
| EP1920785A1 (en) | 2006-11-07 | 2008-05-14 | Boehringer Ingelheim Vetmedica Gmbh | Liquid preparation comprising a complex of pimobendan and cyclodextrin |
| EP2825159B1 (en) | 2012-03-15 | 2022-06-22 | Boehringer Ingelheim Vetmedica GmbH | Pharmaceutical tablet formulation for the veterinary medical sector, method of production and use thereof |
| SI3865120T1 (en) | 2013-07-19 | 2025-12-31 | Boehringer Ingelheim Vetmedica Gmbh | Preserved etherified cyclodextrin derivatives containing liquid aqueous pharmaceutical composition |
| BR112016011111B1 (en) | 2013-12-04 | 2022-11-16 | Boehringer Ingelheim Vetmedica Gmbh | IMPROVED PHARMACEUTICAL COMPOSITIONS OF PIMOBENDAN |
| US10537570B2 (en) | 2016-04-06 | 2020-01-21 | Boehringer Ingelheim Vetmedica Gmbh | Use of pimobendan for the reduction of heart size and/or the delay of onset of clinical symptoms in patients with asymptomatic heart failure due to mitral valve disease |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4316906A (en) * | 1978-08-11 | 1982-02-23 | E. R. Squibb & Sons, Inc. | Mercaptoacyl derivatives of substituted prolines |
| GB9013750D0 (en) * | 1990-06-20 | 1990-08-08 | Pfizer Ltd | Therapeutic agents |
| GB9401090D0 (en) * | 1994-01-21 | 1994-03-16 | Glaxo Lab Sa | Chemical compounds |
| US6143746A (en) * | 1994-01-21 | 2000-11-07 | Icos Corporation | Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use |
| IL135462A0 (en) * | 1997-11-12 | 2001-05-20 | Bayer Ag | 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors |
| HK1049834A1 (en) * | 1999-10-11 | 2003-05-30 | 辉瑞大药厂 | 5-(2-substituted-5-heterocyclylsulphonylpyrid-3-yl)-dihydropyrazolo[4,3-d]pyrimidin-7-ones as phosphodiesterase inhibitors |
| 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 |
-
2003
- 2003-05-09 CN CNA038118262A patent/CN1655820A/en active Pending
- 2003-05-09 WO PCT/IB2003/001889 patent/WO2003099194A2/en not_active Ceased
- 2003-05-09 KR KR10-2004-7018868A patent/KR20050004195A/en not_active Abandoned
- 2003-05-09 RU RU2004133973/15A patent/RU2004133973A/en not_active Application Discontinuation
- 2003-05-09 BR BR0311191-1A patent/BR0311191A/en not_active IP Right Cessation
- 2003-05-09 MX MXPA04010951A patent/MXPA04010951A/en unknown
- 2003-05-09 AU AU2003223071A patent/AU2003223071A1/en not_active Abandoned
- 2003-05-09 PL PL03374198A patent/PL374198A1/en not_active Application Discontinuation
- 2003-05-09 JP JP2004506721A patent/JP2005529927A/en not_active Abandoned
- 2003-05-09 EP EP03719042A patent/EP1506015A2/en not_active Withdrawn
- 2003-05-09 CA CA002485984A patent/CA2485984A1/en not_active Abandoned
- 2003-05-12 TW TW092112826A patent/TW200407153A/en unknown
- 2003-05-19 PE PE2003000482A patent/PE20040514A1/en not_active Application Discontinuation
- 2003-05-21 AR ARP030101762A patent/AR040090A1/en unknown
- 2003-05-21 UY UY27816A patent/UY27816A1/en not_active Application Discontinuation
- 2003-05-22 PA PA20038574201A patent/PA8574201A1/en unknown
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2004
- 2004-11-01 IL IL16497504A patent/IL164975A0/en unknown
- 2004-12-17 NO NO20045517A patent/NO20045517L/en not_active Application Discontinuation
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| PL374198A1 (en) | 2005-10-03 |
| KR20050004195A (en) | 2005-01-12 |
| TW200407153A (en) | 2004-05-16 |
| CA2485984A1 (en) | 2003-12-04 |
| RU2004133973A (en) | 2005-09-10 |
| MXPA04010951A (en) | 2005-06-08 |
| EP1506015A2 (en) | 2005-02-16 |
| UY27816A1 (en) | 2003-12-31 |
| CN1655820A (en) | 2005-08-17 |
| PE20040514A1 (en) | 2004-08-24 |
| BR0311191A (en) | 2005-03-01 |
| JP2005529927A (en) | 2005-10-06 |
| IL164975A0 (en) | 2005-12-18 |
| PA8574201A1 (en) | 2003-12-19 |
| WO2003099194A2 (en) | 2003-12-04 |
| NO20045517L (en) | 2004-12-17 |
| AU2003223071A1 (en) | 2003-12-12 |
| WO2003099194A3 (en) | 2004-06-03 |
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