ECSP13012852A - Derivados de 6-ciclobutil-1,5-dihidro-pirazolo [3,4-d]pirimidin-4-ona y su uso como inhibidores de pde9a. - Google Patents
Derivados de 6-ciclobutil-1,5-dihidro-pirazolo [3,4-d]pirimidin-4-ona y su uso como inhibidores de pde9a.Info
- Publication number
- ECSP13012852A ECSP13012852A ECSP13012852A ECSP13012852A EC SP13012852 A ECSP13012852 A EC SP13012852A EC SP13012852 A ECSP13012852 A EC SP13012852A EC SP13012852 A ECSP13012852 A EC SP13012852A
- Authority
- EC
- Ecuador
- Prior art keywords
- cycllobutil
- pirazolo
- pirimidin
- dihidro
- ona
- Prior art date
Links
- 229940122229 Phosphodiesterase 9A inhibitor Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 229940079593 drug Drugs 0.000 abstract 3
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 101100407341 Drosophila melanogaster Pde9 gene Proteins 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 230000007812 deficiency Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000028252 learning or memory Effects 0.000 abstract 1
- 230000008447 perception Effects 0.000 abstract 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 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl 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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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
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- 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
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Reproductive Health (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Anesthesiology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La invención se refiere a nuevas pirazolopirimidinonas de acuerdo con la fórmula (I). (I),en la que R1 es un grupo piridilo o pirimidinilo y D es ciclopentilo, ciclohexilo, tetrahidrofuranilo, tetrahidropiranilo o 2-, 3- o 4-piridilo opcionalmente sustituidos.Los nuevos compuestos se usan como la entidad activa de medicamentos o para la fabricación de medicamentos respectivamente, en particular medicamentos para el tratamiento de afecciones relacionadas con deficiencias en la percepción, concentración, aprendizaje o memoria. Dichas afecciones pueden estar asociadas por ejemplo con la enfermedad de Alzheimer, esquizofrenia y otras enfermedades. Los nuevos compuestos son también, por ejemplo, para la fabricación de medicamentos y/o para usar en el tratamiento de estas enfermedades, en particular para el deterioro cognitivo asociado con dicha enfermedad. Los compuestos de la invención muestran propiedades inhibidoras de la PDE9.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11154397 | 2011-02-14 | ||
| PCT/EP2011/063705 WO2012020022A1 (en) | 2010-08-12 | 2011-08-09 | 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP13012852A true ECSP13012852A (es) | 2014-09-30 |
Family
ID=46671960
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP13012852 ECSP13012852A (es) | 2011-02-14 | 2013-08-26 | Derivados de 6-ciclobutil-1,5-dihidro-pirazolo [3,4-d]pirimidin-4-ona y su uso como inhibidores de pde9a. |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US20130040971A1 (es) |
| EP (1) | EP2675807B1 (es) |
| JP (1) | JP2014505091A (es) |
| KR (1) | KR20140010036A (es) |
| CN (1) | CN103459397A (es) |
| AP (1) | AP2013007045A0 (es) |
| AR (1) | AR085219A1 (es) |
| AU (1) | AU2012217208A1 (es) |
| BR (1) | BR112013020605A2 (es) |
| CA (1) | CA2827261A1 (es) |
| CL (1) | CL2013002341A1 (es) |
| CO (1) | CO6791616A2 (es) |
| EA (1) | EA023574B1 (es) |
| EC (1) | ECSP13012852A (es) |
| IL (1) | IL227526A0 (es) |
| MA (1) | MA34889B1 (es) |
| MX (1) | MX2013009343A (es) |
| PE (1) | PE20140970A1 (es) |
| PH (1) | PH12013501677A1 (es) |
| SG (1) | SG192756A1 (es) |
| TN (1) | TN2013000324A1 (es) |
| TW (1) | TW201245199A (es) |
| WO (1) | WO2012110440A1 (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10238722A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse |
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| 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 |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害活性を有する２－アミノピリミジン－４－オンおよび２－アミノピリジン誘導体 |
| UY32531A (es) | 2009-03-31 | 2010-10-29 | Boehringer Ingelheim Int | Nuevos compuestos para el tratamiento de trastornos del snc |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| CA2816285A1 (en) | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| CN105669680B (zh) * | 2016-03-24 | 2018-02-23 | 南京药捷安康生物科技有限公司 | 吡咯并[2,1‑f][1,2,4]三嗪‑4(1H)‑酮衍生物类PDE9A抑制剂 |
| BR112019023569A2 (pt) | 2017-06-01 | 2020-06-02 | Eisai R&D Management Co., Ltd. | Agente terapêutico da demência combinando derivados de pirazoloquinolina e donepezila |
| JP7177772B2 (ja) | 2017-06-01 | 2022-11-24 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピラゾロキノリン誘導体とメマンチンの併用による認知症治療剤 |
| CN116585316A (zh) | 2017-06-01 | 2023-08-15 | 卫材R&D管理有限公司 | 包含pde9抑制剂的药物组合物 |
| KR20200010220A (ko) | 2017-06-01 | 2020-01-30 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 피라졸로퀴놀린 유도체를 함유하는 루이소체 질병 치료제 |
| JP2020523309A (ja) * | 2017-06-08 | 2020-08-06 | 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． | ピラゾロピリミジンｐｄｅ９インヒビター |
| EP3893881B1 (en) | 2018-12-12 | 2024-10-09 | Merck Sharp & Dohme LLC | Cyclobutyl pyrazolopyrimidine pde9 inhibitors |
| CN110339197A (zh) * | 2019-06-24 | 2019-10-18 | 中山大学 | 一种防治血管性痴呆的磷酸二酯酶9a抑制剂的用途 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH396924A (de) | 1960-05-11 | 1965-08-15 | Ciba Geigy | Verfahren zur Herstellung von 4-Mercapto-pyrazolo(3,4-d)pyrimidinen |
| DE1147234B (de) | 1960-05-11 | 1963-04-18 | Ciba Geigy | Verfahren zur Herstellung von 1-Isopropyl-4-hydroxy-6-benzyl-pyrazolo[3, 4-d]pyrimidin |
| CH396927A (de) | 1960-05-11 | 1965-08-15 | Ciba Geigy | Verfahren zur Herstellung neuer Pyrazolopyrimidine |
| DE1149013B (de) | 1960-05-11 | 1963-05-22 | Ciba Geigy | Verfahren zur Herstellung von 4-Oxo-4, 5-dihydro-pyrazolo-[3, 4-d]Pyrimidinen |
| CH396926A (de) | 1960-05-11 | 1965-08-15 | Ciba Geigy | Verfahren zur Herstellung neuer Pyrazolopyrimidine |
| CH396925A (de) | 1960-05-11 | 1965-08-15 | Ciba Geigy | Verfahren zur Herstellung neuer Pyrazolopyrimidine |
| US3732225A (en) | 1970-07-23 | 1973-05-08 | Squibb & Sons Inc | Pyrazolo(3,4-d)pyrimidine derivatives |
| US3847908A (en) | 1973-03-05 | 1974-11-12 | Squibb & Sons Inc | 6-styrylpyrazolo(3,4-d)pyrimidinones and pyrimidines |
| ES2203635T3 (es) | 1994-04-27 | 2004-04-16 | Novartis Ag | Nucleosidos y oligonucleotidos con grupos 2'-eter. |
| AU727177B2 (en) | 1996-10-16 | 2000-12-07 | Icn Pharmaceuticals, Inc. | Purine L-nucleosides, analogs and uses thereof |
| DE19709877A1 (de) | 1997-03-11 | 1998-09-17 | Bayer Ag | 1,5-Dihydro-pyrazolo[3,4-d]-pyrimidinon-derivate |
| SK11922002A3 (sk) | 2000-02-18 | 2003-06-03 | Shire Biochem Inc. | Použitie analógov nukleozidov na liečenie alebo prevenciu infekcií spôsobených flavivírusom |
| EP1313478A2 (en) * | 2000-08-30 | 2003-05-28 | Lilly Icos LLC | Method for treatment of migraine using pde5 inhibitors |
| MXPA03006514A (es) | 2001-01-22 | 2004-12-02 | Merck & Co Inc | Derivados de nucleosidos como inhibidores de polimerasa de acido ribonucleico viral dependiente de acido ribonucleico. |
| WO2004009921A2 (en) | 2002-07-19 | 2004-01-29 | Mossor David B | Portable shielding system |
| DE10238722A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse |
| DE10238724A1 (de) | 2002-08-23 | 2004-03-04 | Bayer Ag | Alkyl-substituierte Pyrazolpyrimidine |
| DE10238723A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Phenyl-substituierte Pyrazolyprimidine |
| US20040220186A1 (en) | 2003-04-30 | 2004-11-04 | Pfizer Inc. | PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease |
| 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 |
| WO2004099211A1 (de) | 2003-05-09 | 2004-11-18 | 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 |
| AU2004293423A1 (en) | 2003-11-21 | 2005-06-09 | University Of Connecticut | Heterocyclyl-substituted oxetanes for the treatment of proliferative or infectious diseases |
| WO2006084281A1 (en) | 2005-02-04 | 2006-08-10 | Millennium Pharmaceuticals, Inc. | Inhibitors of e1 activating enzymes |
| PT2152712E (pt) * | 2007-05-11 | 2012-02-29 | Pfizer | Compostos amino-heterocíclicos |
| US8648085B2 (en) | 2007-11-30 | 2014-02-11 | Boehringer Ingelheim International Gmbh | 1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders |
| 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 |
| CN102143965A (zh) * | 2008-09-08 | 2011-08-03 | 贝林格尔.英格海姆国际有限公司 | 吡唑并嘧啶酮及其在治疗中枢神经系统疾病中的用途 |
| UY32531A (es) | 2009-03-31 | 2010-10-29 | Boehringer Ingelheim Int | Nuevos compuestos para el tratamiento de trastornos del snc |
| AR077859A1 (es) * | 2009-08-12 | 2011-09-28 | Boehringer Ingelheim Int | Compuestos para el tratamiento de trastornos del snc |
| BR112013003097B1 (pt) * | 2010-08-12 | 2021-03-16 | Boehringer Ingelheim International Gmbh | 6-cicloalquil-pirazolopirimidinonas e composição farmacêutica |
-
2012
- 2012-02-09 US US13/369,623 patent/US20130040971A1/en not_active Abandoned
- 2012-02-13 CN CN2012800177072A patent/CN103459397A/zh active Pending
- 2012-02-13 SG SG2013061494A patent/SG192756A1/en unknown
- 2012-02-13 PE PE2013001871A patent/PE20140970A1/es not_active Application Discontinuation
- 2012-02-13 WO PCT/EP2012/052378 patent/WO2012110440A1/en not_active Ceased
- 2012-02-13 MX MX2013009343A patent/MX2013009343A/es active IP Right Grant
- 2012-02-13 KR KR1020137021400A patent/KR20140010036A/ko not_active Withdrawn
- 2012-02-13 AR ARP120100472A patent/AR085219A1/es unknown
- 2012-02-13 AP AP2013007045A patent/AP2013007045A0/xx unknown
- 2012-02-13 MA MA36160A patent/MA34889B1/fr unknown
- 2012-02-13 JP JP2013552980A patent/JP2014505091A/ja active Pending
- 2012-02-13 TW TW101104596A patent/TW201245199A/zh unknown
- 2012-02-13 EA EA201300908A patent/EA023574B1/ru not_active IP Right Cessation
- 2012-02-13 BR BR112013020605A patent/BR112013020605A2/pt not_active IP Right Cessation
- 2012-02-13 AU AU2012217208A patent/AU2012217208A1/en not_active Abandoned
- 2012-02-13 PH PH1/2013/501677A patent/PH12013501677A1/en unknown
- 2012-02-13 EP EP20120705246 patent/EP2675807B1/en active Active
- 2012-02-13 CA CA2827261A patent/CA2827261A1/en not_active Abandoned
-
2013
- 2013-07-18 IL IL227526A patent/IL227526A0/en unknown
- 2013-07-29 TN TNP2013000324A patent/TN2013000324A1/fr unknown
- 2013-08-12 CL CL2013002341A patent/CL2013002341A1/es unknown
- 2013-08-26 EC ECSP13012852 patent/ECSP13012852A/es unknown
- 2013-09-12 CO CO13216891A patent/CO6791616A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW201245199A (en) | 2012-11-16 |
| EA023574B1 (ru) | 2016-06-30 |
| AR085219A1 (es) | 2013-09-18 |
| EA201300908A1 (ru) | 2014-01-30 |
| TN2013000324A1 (en) | 2015-01-20 |
| CA2827261A1 (en) | 2012-08-23 |
| WO2012110440A9 (en) | 2013-03-14 |
| WO2012110440A1 (en) | 2012-08-23 |
| JP2014505091A (ja) | 2014-02-27 |
| SG192756A1 (en) | 2013-09-30 |
| MA34889B1 (fr) | 2014-02-01 |
| CL2013002341A1 (es) | 2014-04-04 |
| MX2013009343A (es) | 2013-10-01 |
| EP2675807A1 (en) | 2013-12-25 |
| BR112013020605A2 (pt) | 2016-10-18 |
| PH12013501677A1 (en) | 2018-04-11 |
| IL227526A0 (en) | 2013-09-30 |
| CN103459397A (zh) | 2013-12-18 |
| AU2012217208A1 (en) | 2013-08-01 |
| AP2013007045A0 (en) | 2013-08-31 |
| KR20140010036A (ko) | 2014-01-23 |
| CO6791616A2 (es) | 2013-11-14 |
| EP2675807B1 (en) | 2015-04-22 |
| US20130040971A1 (en) | 2013-02-14 |
| PE20140970A1 (es) | 2014-08-03 |
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