JP2004506009A5 - - Google Patents

Info

Publication number

JP2004506009A5

JP2004506009A5 JP2002518944A JP2002518944A JP2004506009A5 JP 2004506009 A5 JP2004506009 A5 JP 2004506009A5 JP 2002518944 A JP2002518944 A JP 2002518944A JP 2002518944 A JP2002518944 A JP 2002518944A JP 2004506009 A5 JP2004506009 A5 JP 2004506009A5

Authority

JP

Japan

Prior art keywords

selective

ethyl

pharmaceutical composition

pde5 inhibitor

pyrazolo

Prior art date

2001-08-06

Legal status (The legal status 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 status listed.)

Withdrawn

Links

• Espacenet
• Global Dossier
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• 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 9
• 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 9
• 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 9
• DOTPSQVYOBAWPQ-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-3-one Chemical compound N1=CN=C2C(=O)N=NC2=C1 DOTPSQVYOBAWPQ-UHFFFAOYSA-N 0.000 claims 9
• 239000008194 pharmaceutical composition Substances 0.000 claims 8
• 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 6
• 239000012453 solvate Substances 0.000 claims 4
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
• 208000002705 Glucose Intolerance Diseases 0.000 claims 3
• 230000001684 chronic effect Effects 0.000 claims 3
• 201000009104 prediabetes syndrome Diseases 0.000 claims 3
• 150000003839 salts Chemical class 0.000 claims 3
• 229960003310 sildenafil Drugs 0.000 claims 3
• 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 claims 2
• 206010022489 Insulin Resistance Diseases 0.000 claims 2
• 239000000203 mixture Substances 0.000 claims 2
• 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
• WJQXYMDJKXVKMF-UHFFFAOYSA-N 3-ethyl-5-[5-(4-ethylpiperazin-1-yl)sulfonyl-2-(2-methoxyethoxy)pyridin-3-yl]-6-methyl-2-pyridin-2-ylpyrazolo[4,3-d]pyrimidin-7-one Chemical compound C1CN(CC)CCN1S(=O)(=O)C1=CN=C(OCCOC)C(C=2N(C(=O)C3=NN(C(CC)=C3N=2)C=2N=CC=CC=2)C)=C1 WJQXYMDJKXVKMF-UHFFFAOYSA-N 0.000 claims 1
• OABVKOFQXWSACK-UHFFFAOYSA-N 3-ethyl-5-[5-(4-ethylpiperazin-1-yl)sulfonyl-2-propoxyphenyl]-6-methyl-2-pyridin-2-ylpyrazolo[4,3-d]pyrimidin-7-one Chemical compound CCCOC1=CC=C(S(=O)(=O)N2CCN(CC)CC2)C=C1C(N(C(=O)C1=N2)C)=NC1=C(CC)N2C1=CC=CC=N1 OABVKOFQXWSACK-UHFFFAOYSA-N 0.000 claims 1
• 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
• -1 4-Ethylpiperazin-1-ylsulfonyl Chemical group 0.000 claims 1
• DYHVWOAZIYHPLL-UHFFFAOYSA-N 5-[2-ethoxy-5-(2-morpholin-4-ylacetyl)phenyl]-1-ethyl-3-propyl-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound CCCC1=NN(CC)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1C(=O)CN1CCOCC1 DYHVWOAZIYHPLL-UHFFFAOYSA-N 0.000 claims 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 claims 1
• 230000001154 acute effect Effects 0.000 claims 1
• 238000013270 controlled release Methods 0.000 claims 1
• 206010012601 diabetes mellitus Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 238000009472 formulation Methods 0.000 claims 1
• 230000002650 habitual effect Effects 0.000 claims 1
• 238000002638 palliative care Methods 0.000 claims 1
• 238000011321 prophylaxis Methods 0.000 claims 1
• 229960002639 sildenafil citrate Drugs 0.000 claims 1
• 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 claims 1
• 238000013268 sustained release Methods 0.000 claims 1
• 239000012730 sustained-release form Substances 0.000 claims 1
• 230000001225 therapeutic effect Effects 0.000 claims 1
• 238000011282 treatment Methods 0.000 claims 1