OA11168A - Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3', 5'-monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction - Google Patents
Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3', 5'-monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction Download PDFInfo
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- OA11168A OA11168A OA9900234A OA9900234A OA11168A OA 11168 A OA11168 A OA 11168A OA 9900234 A OA9900234 A OA 9900234A OA 9900234 A OA9900234 A OA 9900234A OA 11168 A OA11168 A OA 11168A
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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 title claims abstract description 22
- 238000011282 treatment Methods 0.000 title abstract description 9
- ZOOGRGPOEVQQDX-UHFFFAOYSA-N cyclic GMP Natural products O1C2COP(O)(=O)OC2C(O)C1N1C=NC2=C1NC(N)=NC2=O ZOOGRGPOEVQQDX-UHFFFAOYSA-N 0.000 title description 15
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 title description 5
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 title description 5
- 201000001880 Sexual dysfunction Diseases 0.000 title description 2
- 231100000872 sexual dysfunction Toxicity 0.000 title description 2
- 101100189582 Dictyostelium discoideum pdeD gene Proteins 0.000 title 1
- 101150098694 PDE5A gene Proteins 0.000 title 1
- 102100029175 cGMP-specific 3',5'-cyclic phosphodiesterase Human genes 0.000 title 1
- DOTPSQVYOBAWPQ-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-3-one Chemical class N1=CN=C2C(=O)N=NC2=C1 DOTPSQVYOBAWPQ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 398
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 29
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 26
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 15
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract description 14
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims abstract description 10
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- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 7
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- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims abstract 6
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- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims description 2
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- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- SGPGESCZOCHFCL-UHFFFAOYSA-N Tilisolol hydrochloride Chemical compound [Cl-].C1=CC=C2C(=O)N(C)C=C(OCC(O)C[NH2+]C(C)(C)C)C2=C1 SGPGESCZOCHFCL-UHFFFAOYSA-N 0.000 claims 3
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- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
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- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
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- DKACXUFSLUYRFU-UHFFFAOYSA-N tert-butyl n-aminocarbamate Chemical compound CC(C)(C)OC(=O)NN DKACXUFSLUYRFU-UHFFFAOYSA-N 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- XJDNKRIXUMDJCW-UHFFFAOYSA-J titanium tetrachloride Chemical compound Cl[Ti](Cl)(Cl)Cl XJDNKRIXUMDJCW-UHFFFAOYSA-J 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- GNMJFQWRASXXMS-UHFFFAOYSA-M trimethyl(phenyl)azanium;bromide Chemical compound [Br-].C[N+](C)(C)C1=CC=CC=C1 GNMJFQWRASXXMS-UHFFFAOYSA-M 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
Classifications
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Gynecology & Obstetrics (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9708406.5A GB9708406D0 (en) | 1997-04-25 | 1997-04-25 | Therapeutic agents |
| GB9715380A GB9715380D0 (en) | 1997-07-22 | 1997-07-22 | Therapeutic agents |
| GBGB9722954.6A GB9722954D0 (en) | 1997-10-30 | 1997-10-30 | Therapeutic agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| OA11168A true OA11168A (en) | 2003-04-28 |
Family
ID=27268823
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| OA9900234A OA11168A (en) | 1997-04-25 | 1999-10-22 | Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3', 5'-monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US6723719B1 (cs) |
| EP (1) | EP0977756A1 (cs) |
| JP (2) | JP3563078B2 (cs) |
| KR (2) | KR100390612B1 (cs) |
| CN (2) | CN1188415C (cs) |
| AP (1) | AP1002A (cs) |
| AR (1) | AR015595A1 (cs) |
| AU (1) | AU730670B2 (cs) |
| BG (1) | BG103828A (cs) |
| BR (1) | BR9810233A (cs) |
| CA (1) | CA2288910C (cs) |
| CO (1) | CO4940472A1 (cs) |
| CZ (1) | CZ299633B6 (cs) |
| DZ (1) | DZ2465A1 (cs) |
| EA (2) | EA004315B1 (cs) |
| HR (1) | HRP980222B1 (cs) |
| ID (1) | ID22834A (cs) |
| IL (5) | IL132276A0 (cs) |
| IS (1) | IS5200A (cs) |
| MA (1) | MA24529A1 (cs) |
| NO (1) | NO314585B1 (cs) |
| NZ (1) | NZ338075A (cs) |
| OA (1) | OA11168A (cs) |
| PA (1) | PA8450401A1 (cs) |
| PE (1) | PE68699A1 (cs) |
| PL (1) | PL336586A1 (cs) |
| RS (1) | RS50118B (cs) |
| SK (1) | SK285991B6 (cs) |
| TN (1) | TNSN98053A1 (cs) |
| TR (1) | TR199902646T2 (cs) |
| WO (1) | WO1998049166A1 (cs) |
Families Citing this family (140)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9423910D0 (en) * | 1994-11-26 | 1995-01-11 | Pfizer Ltd | Therapeutic agents |
| IL120266A (en) | 1996-02-28 | 2005-05-17 | Pfizer | Use of estrogen antagonists and estrogen agonists in the preparation of medicaments for inhibiting pathological conditions |
| GB9612514D0 (en) * | 1996-06-14 | 1996-08-14 | Pfizer Ltd | Novel process |
| US6331543B1 (en) | 1996-11-01 | 2001-12-18 | Nitromed, Inc. | Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use |
| ID22834A (id) | 1997-04-25 | 1999-12-09 | Pfizer | Pirazolopimidinona untuk kelainan seksual |
| GB9722520D0 (en) | 1997-10-24 | 1997-12-24 | Pfizer Ltd | Compounds |
| EP1073658B1 (en) | 1998-04-20 | 2003-08-13 | Pfizer Inc. | Pyrazolopyrimidinone cgmp pde5 inhibitors for the treatment of sexual dysfunction |
| DE19827640A1 (de) | 1998-06-20 | 1999-12-23 | Bayer Ag | 7-Alkyl- und Cycloalkyl-substituierte Imidazotriazinone |
| GB9822238D0 (en) * | 1998-10-12 | 1998-12-09 | Pfizer Ltd | Process for preparation of pyrazolo[4,3-D]pyrimidin-7-ones and intermediates thereof |
| GB9823103D0 (en) | 1998-10-23 | 1998-12-16 | Pfizer Ltd | Pharmaceutically active compounds |
| GB9823102D0 (en) | 1998-10-23 | 1998-12-16 | Pfizer Ltd | Pharmaceutically active compounds |
| GB9823101D0 (en) * | 1998-10-23 | 1998-12-16 | Pfizer Ltd | Pharmaceutically active compounds |
| RU2220145C2 (ru) * | 1998-11-11 | 2003-12-27 | Донг А Фарм. Ко., Лтд. | Производные пиразолопиримидинона для лечения импотенции и способ их получения |
| KR100353014B1 (ko) * | 1998-11-11 | 2002-09-18 | 동아제약 주식회사 | 발기부전 치료에 효과를 갖는 피라졸로피리미디논 화합물 |
| US6225315B1 (en) | 1998-11-30 | 2001-05-01 | Pfizer Inc | Method of treating nitrate-induced tolerance |
| WO2000066114A1 (en) * | 1999-04-30 | 2000-11-09 | Lilly Icos Llc | Treatment of female arousal disorder |
| ES2187234A1 (es) * | 1999-04-30 | 2003-05-16 | Lilly Icos Llc | Forma de dosificacion oral para tratar la disfuncion sexual. |
| US6242444B1 (en) | 1999-06-04 | 2001-06-05 | The Jordanian Pharmaceutical Manufacturing And Medical Equipment Co., Ltd. | Compounds and pharmaceutical compositions containing the same |
| ATE228134T1 (de) * | 1999-06-04 | 2002-12-15 | Jordanian Pharmaceutical Mfg A | Kondensierte pyrimidinderivate und diese enthaltende pharmazeutische zubereitungen |
| ES2166270B1 (es) * | 1999-07-27 | 2003-04-01 | Almirall Prodesfarma Sa | Derivados de 8-fenil-6,9-dihidro-(1,2,4,)triazolo(3,4-i)purin-5-ona. |
| DE19942474A1 (de) * | 1999-09-06 | 2001-03-15 | Merck Patent Gmbh | Pyrazolo[4,3-d]pyrimidine |
| YU59100A (sh) * | 1999-10-11 | 2003-10-31 | Pfizer Inc. | Postupak za dobijanje pirazolo (4,3-d) pirimidin-7-ona-3-piridilsulfonil jedinjenja i njihova intermedijera |
| IL149025A0 (en) | 1999-10-11 | 2002-11-10 | Pfizer | 5-(2-substituted-5-heterocyclylsulphonylpyrid-3-yl)-dihydropyrazolo [4, 3-d] pyrimidin-7-ones as phosphodiesterase inhibitors |
| US6350751B1 (en) | 1999-10-11 | 2002-02-26 | Pfizer Inc. | Therapeutic agents |
| GB9923968D0 (en) * | 1999-10-11 | 1999-12-15 | Pfizer Ltd | Therapeutic agents |
| 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 |
| TW200400821A (en) * | 1999-11-02 | 2004-01-16 | Pfizer | Pharmaceutical composition (II) useful for treating or preventing pulmonary hypertension in a patient |
| EP1261609B1 (de) * | 1999-12-24 | 2004-11-03 | Bayer HealthCare AG | Triazolotriazinone und ihre verwendung |
| BR0017043A (pt) * | 1999-12-24 | 2003-01-07 | Bayer Ag | Imidazo[1,3,5]triazinonas e sua aplicação |
| KR100358083B1 (ko) * | 2000-02-17 | 2002-10-25 | 에스케이케미칼주식회사 | 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도 |
| WO2001087888A1 (en) * | 2000-05-17 | 2001-11-22 | Sk Chemicals Co., Ltd. | Pyrazolopyrimidinone derivatives, process for their preparation and their use |
| KR100377782B1 (ko) * | 2000-06-23 | 2003-03-29 | 동아제약 주식회사 | 발기부전 치료에 효과를 갖는 피라졸로피리미디논화합물의 제조방법 |
| EP1176142A1 (en) * | 2000-07-28 | 2002-01-30 | Pfizer Inc. | Process for the preparation of pyrazoles |
| US6407259B1 (en) | 2000-07-28 | 2002-06-18 | Pfizer Inc. | Process for the preparation of pyrazoles |
| KR20030023747A (ko) * | 2000-08-11 | 2003-03-19 | 화이자 인코포레이티드 | 인슐린 저항성 증후군의 치료 |
| PE20020394A1 (es) | 2000-08-18 | 2002-06-21 | Agouron Pharma | Compuestos de pirazol y composiciones farmaceuticas que los contienen, que modulan y/o inhiben la actividad de erab/hadh2 |
| AU2000267375A1 (en) * | 2000-08-23 | 2002-03-04 | Lg Life Sciences Ltd. | Polyethoxylated pyrazolo pyrimidinone derivatives, process for preparation thereof and pharmaceutical compositions comprising the same for the treatment of impotence |
| US6821978B2 (en) | 2000-09-19 | 2004-11-23 | Schering Corporation | Xanthine phosphodiesterase V inhibitors |
| US6548508B2 (en) | 2000-10-20 | 2003-04-15 | Pfizer, Inc. | Use of PDE V inhibitors for improved fecundity in mammals |
| GB0025782D0 (en) * | 2000-10-20 | 2000-12-06 | Pfizer Ltd | Use of inhibitors |
| SE0004780D0 (sv) | 2000-12-22 | 2000-12-22 | Jordanian Pharmaceutical Mfg & | Novel compunds |
| JP2005509038A (ja) | 2001-11-09 | 2005-04-07 | シェーリング コーポレイション | 多環式グアニン誘導体ホスホジエステラーゼｖ阻害剤 |
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| ATE478872T1 (de) * | 2002-03-28 | 2010-09-15 | Ustav Ex Botan Av Cr V V I I O | Pyrazoloä4,3-düpyrimidine, verfahren zu ihrer herstellung und therapeutische anwendung |
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| DE60332387D1 (de) | 2002-12-13 | 2010-06-10 | Warner Lambert Co | Alpha-2-delta-ligand zur behandlung vonsymptomen der unteren harnwege |
| MXPA05011643A (es) | 2003-04-29 | 2005-12-15 | Pfizer Ltd | 5,7-diaminopirazolo[4,3-d]pirimidinas en el tratamiento de hipertension. |
| PL2256106T3 (pl) | 2003-07-22 | 2015-08-31 | Astex Therapeutics Ltd | Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3) |
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| US8580801B2 (en) | 2008-07-23 | 2013-11-12 | Robert I. Henkin | Phosphodiesterase inhibitor treatment |
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