AR037329A1 - Compuestos pirazolo pirimidinona, procedimientos para la preparacion de los mismos, composiciones farmaceuticas de los mismos y usos de los mismos en la preparacion de medicamentos - Google Patents
Compuestos pirazolo pirimidinona, procedimientos para la preparacion de los mismos, composiciones farmaceuticas de los mismos y usos de los mismos en la preparacion de medicamentosInfo
- Publication number
- AR037329A1 AR037329A1 ARP020104152A ARP020104152A AR037329A1 AR 037329 A1 AR037329 A1 AR 037329A1 AR P020104152 A ARP020104152 A AR P020104152A AR P020104152 A ARP020104152 A AR P020104152A AR 037329 A1 AR037329 A1 AR 037329A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- independently selected
- same
- preparation
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- -1 pyrazol pyrimidinone compound Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- GJCOSYZMQJWQCA-UHFFFAOYSA-N 9H-xanthene Chemical compound C1=CC=C2CC3=CC=CC=C3OC2=C1 GJCOSYZMQJWQCA-UHFFFAOYSA-N 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 1
- QDLAGTHXVHQKRE-UHFFFAOYSA-N lichenxanthone Natural products COC1=CC(O)=C2C(=O)C3=C(C)C=C(OC)C=C3OC2=C1 QDLAGTHXVHQKRE-UHFFFAOYSA-N 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D487/04—Ortho-condensed systems
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Ophthalmology & Optometry (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Pregnancy & Childbirth (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Otolaryngology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Toxicology (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un compuesto pirazolo pirimidinona de acuerdo con la fórmula (1), una sal, un solvato o profármaco farmacéuticamente aceptable de éste, en el que: R1 es H o alquilo C1-6 en el que R1 se une bien a N1 o N2; R2 es alquilo C1-6 opcionalmente sustituido con hidroxi o alcoxi; cicloalquilo C3-7 opcionalmente sustituido con alquilo, hidroxi o alcoxi; un heterociclo saturado de 5-6 miembros opcionalmente sustituido con alquilo, hidroxi o alcoxi, het1 o Ar1; R3 es alquilo C1-6 opcionalmente sustituido con 1 ó 2 grupos independientemente seleccionados entre: Ar2, cicloalquilo C3-7 opcionalmente sustituido con alquilo C1-6; OAr2, SAr2; NHC(O) alquilo C1-6; het2; xanteno; y naftaleno; en los que Ar1 y Ar2 son independientemente grupos de fórmula (2), en la que R4, R5 y R6 se seleccionan independientemente de entre: hidrógeno, halo, fenoxi, fenilo, CF3, OCF3, R7, SR7 y OR7, en los que R7 es alquilo C1-6 opcionalmente sustituido con het3 o por un grupo fenilo opcionalmente sustituido con 1, 2 ó 3 grupos independientemente seleccionados entre halo, CF3, OCF3, alquilo C1-6 y alcoxi C1-6: o en la que R4 y R5 se combinan para formar una unión de 3 ó 4 átomos, y en la citada unión se pueden incorporar 1 ó 2 heteroátomos independientemente seleccionados entre O, S y N; y en el que het1, het2 y het3, que pueden ser iguales o distintos, son heterociclos aromáticos de 5-6 miembros que contienen 1, 2 ó 3 heteroátomos, independientemente seleccionados entre O, S y N, los citados heterociclos opcionalmente sustituidos por 1, 2 ó 3 sustituyentes, se seleccionan independientemente entre alquilo C1-6, halo y fenilo opcionalmente sustituido con 1, 2 ó 3 grupos independientemente seleccionados entre halo y alquilo C1-6; con las condiciones de que cuando: a) R1 está unido a N1, R1 es alquilo C1-6 y R2 es propilo, entonces R3 no es etilo sustituido con Ar1, y b) esta unido a N1, R1 es alquilo C1-6 y R2 es metilo, entonces R3 no es alquilo C1-4 sustituido con Ar1, procedimientos para la preparación de los mismos, composiciones farmacéuticas de los mismos y uso de los mismos en la preparación de medicamentos útiles para tratar trastornos cardiovasculares.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0126395A GB0126395D0 (en) | 2001-11-02 | 2001-11-02 | Pyrazolo[4,3]pyrimidine derivatives and their use in treating disease |
| GB0130695A GB0130695D0 (en) | 2001-12-21 | 2001-12-21 | Pyrazola[4,3]pyrimidine |
| GB0216761A GB0216761D0 (en) | 2002-07-18 | 2002-07-18 | PDE9 Inhibitors for treating cardiovascular disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037329A1 true AR037329A1 (es) | 2004-11-03 |
Family
ID=27256310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020104152A AR037329A1 (es) | 2001-11-02 | 2002-10-31 | Compuestos pirazolo pirimidinona, procedimientos para la preparacion de los mismos, composiciones farmaceuticas de los mismos y usos de los mismos en la preparacion de medicamentos |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1440073A1 (es) |
| JP (1) | JP2005511575A (es) |
| AR (1) | AR037329A1 (es) |
| BR (1) | BR0214096A (es) |
| CA (1) | CA2466824A1 (es) |
| DO (1) | DOP2002000482A (es) |
| HN (1) | HN2002000317A (es) |
| MX (1) | MXPA04004171A (es) |
| PA (1) | PA8557401A1 (es) |
| PE (1) | PE20030702A1 (es) |
| SV (1) | SV2004001373A (es) |
| TW (1) | TW200300081A (es) |
| UY (1) | UY27522A1 (es) |
| WO (1) | WO2003037899A1 (es) |
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2459161A1 (en) | 2001-08-31 | 2003-03-13 | The Rockefeller University | Phosphodiesterase activity and regulation of phosphodiesterase 1b-mediated signaling in brain |
| EP1481077B1 (en) * | 2001-12-06 | 2009-11-04 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| DE10238723A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Phenyl-substituierte Pyrazolyprimidine |
| DE10238724A1 (de) | 2002-08-23 | 2004-03-04 | Bayer Ag | Alkyl-substituierte Pyrazolpyrimidine |
| DE10238722A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse |
| US7141669B2 (en) | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod receptor ligands and uses thereof |
| EP1626971B1 (de) * | 2003-05-09 | 2011-08-10 | Boehringer Ingelheim International Gmbh | 6-cyclylmethyl- und 6-alkylmethyl-substituierte pyrazolopyrimidine |
| US8044060B2 (en) | 2003-05-09 | 2011-10-25 | Boehringer Ingelheim International Gmbh | 6-cyclylmethyl- and 6-alkylmethyl pyrazolo[3,4-D]pyrimidines, methods for their preparation and methods for their use to treat impairments of perception, concentration learning and/or memory |
| DE102004004142A1 (de) * | 2003-05-09 | 2004-11-25 | Bayer Healthcare Ag | 6-Cyclylmethyl- und 6-Alkylmethyl-substituierte Pyrazolopyrimidine |
| DE10320785A1 (de) * | 2003-05-09 | 2004-11-25 | Bayer Healthcare Ag | 6-Arylmethyl-substituierte Pyrazolopyrimidine |
| DE10328479A1 (de) * | 2003-06-25 | 2005-01-13 | Bayer Ag | 6-Arylamino-5-cyano-4-pyrimidinone |
| CA2532965C (en) | 2003-07-22 | 2013-05-14 | Astex Therapeutics Limited | 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators |
| DE102004001873A1 (de) | 2004-01-14 | 2005-09-29 | Bayer Healthcare Ag | Cyanopyrimidinone |
| EP1734963A4 (en) | 2004-04-02 | 2008-06-18 | Merck & Co Inc | METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER |
| US7067659B2 (en) * | 2004-04-23 | 2006-06-27 | Duke University | Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof |
| AR054425A1 (es) * | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| DE102005024494A1 (de) * | 2005-05-27 | 2006-11-30 | Bayer Healthcare Ag | Verwendung von Cyanopyrimidinen |
| JP5140418B2 (ja) | 2005-06-14 | 2013-02-06 | あすか製薬株式会社 | チエノピリミジン誘導体 |
| EP1919287A4 (en) * | 2005-08-23 | 2010-04-28 | Intra Cellular Therapies Inc | ORGANIC COMPOUNDS FOR TREATING A REDUCED DOPAMINE RECEPTOR SIGNALING ACTIVITY |
| KR20090042227A (ko) | 2006-06-06 | 2009-04-29 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| ES2581573T3 (es) * | 2006-08-08 | 2016-09-06 | Aska Pharmaceutical Co., Ltd. | Derivado de quinazolina |
| KR101555384B1 (ko) * | 2006-12-13 | 2015-09-23 | 아스카 세이야쿠 가부시키가이샤 | 퀴녹살린 유도체 |
| WO2008072778A1 (ja) * | 2006-12-13 | 2008-06-19 | Aska Pharmaceutical Co., Ltd. | 尿路系疾患の処置剤 |
| US8383852B2 (en) * | 2007-02-16 | 2013-02-26 | Emisphere Technologies, Inc. | Compounds having a cyclic moiety and compositions for delivering active agents |
| DK2152712T3 (da) * | 2007-05-11 | 2012-03-26 | Pfizer | Aminoheterocykliske fobindelser |
| PE20091211A1 (es) * | 2007-11-30 | 2009-09-14 | Boehringer Ingelheim Int | Derivados de pirazolopirimidina como moduladores de pde9a |
| AU2008331833A1 (en) | 2007-12-06 | 2009-06-11 | Intra-Cellular Therapies, Inc | Organic compounds |
| UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| CA2736304A1 (en) | 2008-09-08 | 2010-03-11 | Boehringer Ingelheim International Gmbh | Pyrazolopyrimidines and their use for the treatment of cns disorders |
| EP2348857B1 (en) | 2008-10-22 | 2016-02-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| AU2009309037A1 (en) | 2008-10-31 | 2010-05-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| WO2010065147A1 (en) | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN102223799A (zh) | 2008-12-06 | 2011-10-19 | 细胞内治疗公司 | 有机化合物 |
| KR20110098731A (ko) | 2008-12-06 | 2011-09-01 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| TWI404721B (zh) * | 2009-01-26 | 2013-08-11 | Pfizer | 胺基－雜環化合物 |
| MX2011009314A (es) | 2009-03-05 | 2011-10-11 | Astellas Pharma Inc | Compuesto de quinoxalina. |
| GEP20146098B (en) | 2009-03-31 | 2014-05-27 | Boehringer Ingelheim Int | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their usage as pde9a modulators |
| WO2011016861A2 (en) | 2009-08-05 | 2011-02-10 | Intra-Cellular Therapies, Inc. | Novel regulatory proteins and inhibitors |
| US8895596B2 (en) | 2010-02-25 | 2014-11-25 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| JP5879336B2 (ja) | 2010-05-31 | 2016-03-08 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 有機化合物 |
| WO2011153135A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2012004900A1 (en) * | 2010-07-09 | 2012-01-12 | Aska Pharmaceutical Co., Ltd. | Thienopyrimidine compounds |
| MX344770B (es) | 2010-08-12 | 2017-01-06 | Boehringer Ingelheim Int Gmbh * | Derivados de 6-cicloalquil-1,5-dihidro-pirazolo (3,4-d) pirimidin-4-onas y su uso como inhibidores de pde9a. |
| KR20130097178A (ko) | 2010-09-07 | 2013-09-02 | 아스텔라스세이야쿠 가부시키가이샤 | 퀴녹살린 화합물 |
| MX2013002584A (es) | 2010-09-07 | 2013-04-29 | Astellas Pharma Inc | Compuesto de pirazoloquinolina. |
| JP5886310B2 (ja) * | 2010-12-06 | 2016-03-16 | グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ | Ｌｐ−ＰＬＡ２により媒介される疾患または状態の処置における使用のためのピリミジノン化合物 |
| US8809345B2 (en) | 2011-02-15 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders |
| MY159058A (en) | 2011-02-25 | 2016-12-15 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agent |
| CN104703987B (zh) * | 2011-10-10 | 2017-05-03 | H.隆德贝克有限公司 | 具有咪唑并吡嗪酮骨架的pde9抑制剂 |
| SG11201403909RA (en) | 2012-01-26 | 2014-10-30 | Lundbeck & Co As H | Pde9 inhibitors with imidazo triazinone backbone |
| EP2880028B1 (en) | 2012-08-02 | 2020-09-30 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| CN102786525B (zh) | 2012-08-08 | 2014-12-17 | 中山大学 | N-取代吡唑并[3,4-d]嘧啶酮类化合物、其制备方法及其应用 |
| JP2016516004A (ja) | 2013-02-22 | 2016-06-02 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | 抗糖尿病二環式化合物 |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| US9546175B2 (en) | 2014-08-07 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Organic compounds |
| BR112018000254A2 (pt) | 2015-07-07 | 2018-09-04 | H Lundbeck As | inibidores de pde9 com cadeia principal de imidazotriazinona e cadeia principal de imidazopirazinona para o tratamento de doenças periféricas |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| US10968232B2 (en) | 2016-12-20 | 2021-04-06 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
| JP7293129B2 (ja) | 2017-06-01 | 2023-06-19 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Ｐｄｅ９阻害剤を含む医薬組成物 |
| US11147803B2 (en) | 2017-06-01 | 2021-10-19 | Eisai R&D Management Co., Ltd. | Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine |
| KR20200010220A (ko) | 2017-06-01 | 2020-01-30 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 피라졸로퀴놀린 유도체를 함유하는 루이소체 질병 치료제 |
| CN110603040B (zh) | 2017-06-01 | 2023-02-28 | 卫材R&D管理有限公司 | 组合吡唑并喹啉衍生物和多奈哌齐的痴呆治疗剂 |
| HUE065709T2 (hu) | 2018-05-25 | 2024-06-28 | Cardurion Pharmaceuticals Inc | 6-[(3S,4S)-4-metil-1-(pirimidin-2-ilmetil)pirrolidin-3-il]-3-tetrahidropirán-4-il-7H-imidazo[1,5-a] pirazin-8-on vegyület monohidrát és kristályos formái |
| MA53501A (fr) | 2018-08-31 | 2021-07-07 | Imara Inc | Inhibiteurs de pde9 pour le traitement de la drépanocytose |
| CA3132895C (en) | 2019-03-08 | 2024-05-14 | Transthera Sciences (Nanjing), Inc. | Uses of phosphodiesterase inhibitors |
| KR20230128450A (ko) * | 2020-10-27 | 2023-09-05 | 카듀리온 파마슈티칼스, 인크. | 심부전 치료를 위한 pde9 억제제 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3939161A (en) * | 1973-10-29 | 1976-02-17 | Abbott Laboratories | 1,3-Dimethyl- 1H-pyrazolo(4,3-D) pyrimidine-7 (6H)-ones |
| US4666908A (en) * | 1985-04-05 | 1987-05-19 | Warner-Lambert Company | 5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use |
| GB9722520D0 (en) * | 1997-10-24 | 1997-12-24 | Pfizer Ltd | Compounds |
| DE19838705A1 (de) * | 1998-08-26 | 2000-03-02 | Bayer Ag | Neue Dihydro-(1,2,3)-triazolo-[4,5-d]pyrimidin-7-one |
| IL139457A0 (en) * | 1999-11-08 | 2001-11-25 | Pfizer | Compounds for the treatment of female sexual dysfunction |
| WO2002062799A1 (en) * | 2001-02-05 | 2002-08-15 | Dr. Reddy's Laboratories Ltd. | Aryl substituted alkylcarboxylic acids as hypocholesterolemic agents |
-
2002
- 2002-10-01 HN HN2002000317A patent/HN2002000317A/es unknown
- 2002-10-09 DO DO2002000482A patent/DOP2002000482A/es unknown
- 2002-10-22 EP EP02777623A patent/EP1440073A1/en not_active Withdrawn
- 2002-10-22 BR BR0214096-9A patent/BR0214096A/pt not_active IP Right Cessation
- 2002-10-22 JP JP2003540180A patent/JP2005511575A/ja active Pending
- 2002-10-22 CA CA002466824A patent/CA2466824A1/en not_active Abandoned
- 2002-10-22 WO PCT/IB2002/004385 patent/WO2003037899A1/en not_active Ceased
- 2002-10-22 MX MXPA04004171A patent/MXPA04004171A/es unknown
- 2002-10-29 PA PA20028557401A patent/PA8557401A1/es unknown
- 2002-10-30 UY UY27522A patent/UY27522A1/es not_active Application Discontinuation
- 2002-10-30 PE PE2002001070A patent/PE20030702A1/es not_active Application Discontinuation
- 2002-10-31 AR ARP020104152A patent/AR037329A1/es unknown
- 2002-11-01 SV SV2002001373A patent/SV2004001373A/es not_active Application Discontinuation
- 2002-11-01 TW TW091132424A patent/TW200300081A/zh unknown
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| HN2002000317A (es) | 2003-05-21 |
| TW200300081A (en) | 2003-05-16 |
| BR0214096A (pt) | 2004-09-28 |
| WO2003037899A1 (en) | 2003-05-08 |
| UY27522A1 (es) | 2003-06-30 |
| EP1440073A1 (en) | 2004-07-28 |
| SV2004001373A (es) | 2004-01-07 |
| PE20030702A1 (es) | 2003-08-21 |
| MXPA04004171A (es) | 2004-09-06 |
| CA2466824A1 (en) | 2003-05-08 |
| PA8557401A1 (es) | 2003-11-12 |
| DOP2002000482A (es) | 2003-05-31 |
| JP2005511575A (ja) | 2005-04-28 |
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