DE60204760T2 - Pyrazolo[4,3-d]pyrimidinon-verbindungen als cgmp pde-inhibitoren - Google Patents
Pyrazolo[4,3-d]pyrimidinon-verbindungen als cgmp pde-inhibitoren Download PDFInfo
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- DE60204760T2 DE60204760T2 DE60204760T DE60204760T DE60204760T2 DE 60204760 T2 DE60204760 T2 DE 60204760T2 DE 60204760 T DE60204760 T DE 60204760T DE 60204760 T DE60204760 T DE 60204760T DE 60204760 T2 DE60204760 T2 DE 60204760T2
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- 239000003112 inhibitor Substances 0.000 title description 30
- 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 description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 173
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- 238000011321 prophylaxis Methods 0.000 claims abstract description 4
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- 238000002360 preparation method Methods 0.000 claims description 64
- 125000001424 substituent group Chemical group 0.000 claims description 48
- 229910052736 halogen Inorganic materials 0.000 claims description 41
- 150000002367 halogens Chemical class 0.000 claims description 40
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims description 32
- 125000003118 aryl group Chemical group 0.000 claims description 30
- 239000003814 drug Substances 0.000 claims description 25
- 229910052757 nitrogen Inorganic materials 0.000 claims description 25
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 17
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 16
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 9
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- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Emergency Medicine (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Pregnancy & Childbirth (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0106561A GB0106561D0 (en) | 2001-03-16 | 2001-03-16 | Pharmaceutically active compounds |
| GB0106651A GB0106651D0 (en) | 2001-03-16 | 2001-03-16 | Pharmaceutically active compounds |
| GB0106651 | 2001-03-16 | ||
| GB0106561 | 2001-03-16 | ||
| PCT/IB2002/000679 WO2002074312A1 (en) | 2001-03-16 | 2002-03-07 | Pyrazolo`4,3-d.pyrimidinone compounds as cgmp pde inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60204760D1 DE60204760D1 (de) | 2005-07-28 |
| DE60204760T2 true DE60204760T2 (de) | 2006-05-18 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60204760T Expired - Fee Related DE60204760T2 (de) | 2001-03-16 | 2002-03-07 | Pyrazolo[4,3-d]pyrimidinon-verbindungen als cgmp pde-inhibitoren |
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| Country | Link |
|---|---|
| EP (1) | EP1372656B1 (enExample) |
| JP (1) | JP2004527510A (enExample) |
| AT (1) | ATE298238T1 (enExample) |
| BR (1) | BR0208078A (enExample) |
| CA (1) | CA2436911A1 (enExample) |
| DE (1) | DE60204760T2 (enExample) |
| ES (1) | ES2241994T3 (enExample) |
| MX (1) | MXPA03006310A (enExample) |
| WO (1) | WO2002074312A1 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
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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 |
| WO2004082667A1 (en) * | 2003-03-17 | 2004-09-30 | Pfizer Products Inc. | Treatment of type 1 diabetes with pde5 inhibitors |
| US7141669B2 (en) | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod receptor ligands and uses thereof |
| BRPI0412259B1 (pt) | 2003-07-22 | 2019-08-20 | Astex Therapeutics Limited | Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica |
| WO2005028480A2 (en) * | 2003-09-03 | 2005-03-31 | Neurogen Corporation | 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| 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. |
| KR20140022114A (ko) | 2005-06-06 | 2014-02-21 | 다케다 야쿠힌 고교 가부시키가이샤 | 유기 화합물 |
| JP5386350B2 (ja) * | 2006-05-31 | 2014-01-15 | タケダ カリフォルニア インコーポレイテッド | グルコキナーゼ活性剤としての、インダゾールおよびイソインドール誘導体 |
| WO2007143705A2 (en) | 2006-06-06 | 2007-12-13 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US9006258B2 (en) | 2006-12-05 | 2015-04-14 | Intra-Cellular Therapies, Inc. | Method of treating female sexual dysfunction with a PDE1 inhibitor |
| CN101969774A (zh) | 2007-12-06 | 2011-02-09 | 细胞内治疗公司 | 有机化合物 |
| EA201170772A1 (ru) * | 2008-12-06 | 2012-03-30 | Интра-Селлулар Терапиз, Инк. | Органические соединения |
| US8697710B2 (en) | 2008-12-06 | 2014-04-15 | Intra-Cellular Therapies, Inc. | Optionally substituted 3-amino-4-(thioxo or imino)-4,5-dihydro-2H-pyrazolo [3,4-d]pyrimidin-6(7H)-ones |
| JP5989993B2 (ja) | 2008-12-06 | 2016-09-07 | 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 |
| CA2740385A1 (en) | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN102231953A (zh) | 2008-12-06 | 2011-11-02 | 细胞内治疗公司 | 有机化合物 |
| KR20110103949A (ko) | 2008-12-06 | 2011-09-21 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| JP2012513464A (ja) | 2008-12-23 | 2012-06-14 | ザ トラスティーズ オブ コロンビア ユニヴァーシティ イン ザ シティ オブ ニューヨーク | ホスホジエステラーゼ阻害剤及びその使用 |
| JP2012526810A (ja) | 2009-05-13 | 2012-11-01 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
| WO2011153135A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2011153138A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| TW201206937A (en) | 2010-05-31 | 2012-02-16 | Intra Cellular Therapies Inc | Organic compounds |
| WO2011153136A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US10561656B2 (en) | 2011-06-10 | 2020-02-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP2956141A4 (en) | 2013-02-17 | 2016-10-26 | Intra Cellular Therapies Inc | NEW USES |
| MX378194B (es) | 2013-03-15 | 2025-03-10 | Intra Cellular Therapies Inc | Compuestos organicos. |
| US9545406B2 (en) | 2013-03-15 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Method of treating a CNS injury with a PDE1 inhibitor |
| US9884872B2 (en) | 2014-06-20 | 2018-02-06 | Intra-Cellular Therapies, Inc. | Organic compounds |
| JP6591530B2 (ja) | 2014-08-07 | 2019-10-16 | 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 |
| US10285992B2 (en) | 2014-08-07 | 2019-05-14 | Intra-Cellular Therapies, Inc. | Combinations of PDE1 inhibitors and NEP inhibitors and associated methods |
| US9546175B2 (en) | 2014-08-07 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Organic compounds |
| KR102332957B1 (ko) | 2014-09-17 | 2021-11-29 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 화합물 및 방법 |
| WO2016192083A1 (en) * | 2015-06-04 | 2016-12-08 | Merck Sharp & Dohme Corp. | Dihydropyrazolopyrimidinone compounds as pde2 inhibitors |
| US10682354B2 (en) | 2016-03-28 | 2020-06-16 | Intra-Cellular Therapies, Inc. | Compositions and methods |
| ES2906107T3 (es) | 2016-09-12 | 2022-04-13 | Intra Cellular Therapies Inc | Usos novedosos |
| US11839614B2 (en) | 2018-01-31 | 2023-12-12 | Intra-Cellular Therapies, Inc. | Methods for treating or mitigating cardiotoxicity characterized by inhibition of adenosine A2 signaling and/or adenosine A2 receptor expression |
| JP7612672B2 (ja) | 2019-09-03 | 2025-01-14 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 新規化合物 |
| US12364695B2 (en) | 2020-06-02 | 2025-07-22 | Intra-Cellular Therapies, Inc. | Methods of treating inflammatory disease |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9114760D0 (en) * | 1991-07-09 | 1991-08-28 | Pfizer Ltd | Therapeutic agents |
| GB9301192D0 (en) * | 1993-06-09 | 1993-06-09 | Trott Francis W | Flower shaped mechanised table |
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2002
- 2002-03-07 MX MXPA03006310A patent/MXPA03006310A/es unknown
- 2002-03-07 EP EP02707031A patent/EP1372656B1/en not_active Expired - Lifetime
- 2002-03-07 DE DE60204760T patent/DE60204760T2/de not_active Expired - Fee Related
- 2002-03-07 BR BR0208078-8A patent/BR0208078A/pt not_active IP Right Cessation
- 2002-03-07 WO PCT/IB2002/000679 patent/WO2002074312A1/en not_active Ceased
- 2002-03-07 JP JP2002573019A patent/JP2004527510A/ja active Pending
- 2002-03-07 AT AT02707031T patent/ATE298238T1/de not_active IP Right Cessation
- 2002-03-07 ES ES02707031T patent/ES2241994T3/es not_active Expired - Lifetime
- 2002-03-07 CA CA002436911A patent/CA2436911A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1372656B1 (en) | 2005-06-22 |
| ES2241994T3 (es) | 2005-11-01 |
| WO2002074312A1 (en) | 2002-09-26 |
| DE60204760D1 (de) | 2005-07-28 |
| CA2436911A1 (en) | 2002-09-26 |
| JP2004527510A (ja) | 2004-09-09 |
| BR0208078A (pt) | 2004-03-02 |
| MXPA03006310A (es) | 2003-09-16 |
| EP1372656A1 (en) | 2004-01-02 |
| ATE298238T1 (de) | 2005-07-15 |
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| Date | Code | Title | Description |
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| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |