EA201300908A1 - ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9A - Google Patents
ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9AInfo
- Publication number
- EA201300908A1 EA201300908A1 EA201300908A EA201300908A EA201300908A1 EA 201300908 A1 EA201300908 A1 EA 201300908A1 EA 201300908 A EA201300908 A EA 201300908A EA 201300908 A EA201300908 A EA 201300908A EA 201300908 A1 EA201300908 A1 EA 201300908A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- drugs
- application
- dihydropyrazolo
- pyrimidin
- cyclobutyl
- Prior art date
Links
- 229940122229 Phosphodiesterase 9A inhibitor Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 abstract 4
- 229940079593 drug Drugs 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
- 230000001575 pathological effect Effects 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
- 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
-
- 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
-
- 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
-
- 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
-
- 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
-
- 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
- A61P25/28—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
-
- 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
-
- 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
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Anesthesiology (AREA)
- Child & Adolescent Psychology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
В заявке описаны новые пиразолопиримидиноны формулы (I)в которой Rобозначает пиридильную или пиримидинильную группу и D обозначает необязательно замещенный циклопентил, циклогексил, тетрагидрофуранил, тетрагидропиранил или 2-, 3- или 4-пиридил. Эти новые соединения предназначены для применения в качестве активного компонента лекарственных средств или для приготовления лекарственных средств соответственно, предпочтительно лекарственных средств, предназначенных для лечения патологических состояний, связанных с недостаточностью восприятия, сосредоточенности, способности к обучению или памяти. Такие патологические состояния могут быть связаны, например, с болезнью Альцгеймера, шизофренией и другими заболеваниями. Эти новые соединения также применимы, например, для приготовления лекарственных средств и/или для применения для лечения этих заболеваний, в частности нарушения познавательной способности, связанного с таким заболеванием. Описанные в заявке соединения обладают способностью ингибировать PDE9.
Applications Claiming Priority (3)
| 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 |
| PCT/EP2012/052378 WO2012110440A1 (en) | 2011-02-14 | 2012-02-13 | 6 - cyclobutyl - 1, 5 - dihydro - pyrazolo [3, 4-d] pyrimidin- 4 - one derivatives their use as pde9a inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201300908A1 true EA201300908A1 (ru) | 2014-01-30 |
| EA023574B1 EA023574B1 (ru) | 2016-06-30 |
Family
ID=46671960
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201300908A EA023574B1 (ru) | 2011-02-14 | 2012-02-13 | ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4-d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9A |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US20130040971A1 (ru) |
| EP (1) | EP2675807B1 (ru) |
| JP (1) | JP2014505091A (ru) |
| KR (1) | KR20140010036A (ru) |
| CN (1) | CN103459397A (ru) |
| AP (1) | AP2013007045A0 (ru) |
| AR (1) | AR085219A1 (ru) |
| AU (1) | AU2012217208A1 (ru) |
| BR (1) | BR112013020605A2 (ru) |
| CA (1) | CA2827261A1 (ru) |
| CL (1) | CL2013002341A1 (ru) |
| CO (1) | CO6791616A2 (ru) |
| EA (1) | EA023574B1 (ru) |
| EC (1) | ECSP13012852A (ru) |
| IL (1) | IL227526A0 (ru) |
| MA (1) | MA34889B1 (ru) |
| MX (1) | MX2013009343A (ru) |
| PE (1) | PE20140970A1 (ru) |
| PH (1) | PH12013501677A1 (ru) |
| SG (1) | SG192756A1 (ru) |
| TN (1) | TN2013000324A1 (ru) |
| TW (1) | TW201245199A (ru) |
| WO (1) | WO2012110440A1 (ru) |
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 |
| EP1942105B8 (en) | 2005-10-25 | 2014-08-13 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivative |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| 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 |
| CN102119161B (zh) | 2008-06-13 | 2015-07-08 | 盐野义制药株式会社 | 具有β分泌酶抑制作用的含硫杂环衍生物 |
| JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 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 |
| CA2757231A1 (en) * | 2009-03-31 | 2010-10-07 | Boehringer Ingelheim International Gmbh | 1-heterocyclyl-1,5-dihydro-pyrazolo [3,4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
| JP5816630B2 (ja) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
| 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 |
| US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
| 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 |
| WO2018221550A1 (ja) | 2017-06-01 | 2018-12-06 | 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 |
| SG11201909359YA (en) | 2017-06-01 | 2019-11-28 | Eisai R&D Man Co Ltd | Pharmaceutical composition comprising pde9 inhibitor |
| JP7269875B2 (ja) | 2017-06-01 | 2023-05-09 | 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を含有するレビー小体病治療剤 |
| RU2019135834A (ru) | 2017-06-01 | 2021-07-13 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Терапевтическое средство для лечения деменции, представляющее собой комбинацию производного пиразолохинолина и донепезила |
| KR20200013758A (ko) * | 2017-06-08 | 2020-02-07 | 머크 샤프 앤드 돔 코포레이션 | 피라졸로피리미딘 pde9 억제제 |
| WO2020123271A1 (en) * | 2018-12-12 | 2020-06-18 | Merck Sharp & Dohme Corp. | 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 |
|---|---|---|---|---|
| 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 |
| 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 |
| CH396924A (de) | 1960-05-11 | 1965-08-15 | Ciba Geigy | Verfahren zur Herstellung von 4-Mercapto-pyrazolo(3,4-d)pyrimidinen |
| CH396925A (de) | 1960-05-11 | 1965-08-15 | Ciba Geigy | Verfahren zur Herstellung neuer Pyrazolopyrimidine |
| CH396927A (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 |
| PT679657E (pt) | 1994-04-27 | 2003-11-28 | Novartis Ag | Nucleosidos e oligonucleotidos com grupos 2'-eter |
| JP2001524936A (ja) | 1996-10-16 | 2001-12-04 | アイ・シー・エヌ・フアーマシユーテイカルズ・インコーポレイテツド | プリンｌ―ヌクレオシド類およびその用途 |
| DE19709877A1 (de) | 1997-03-11 | 1998-09-17 | Bayer Ag | 1,5-Dihydro-pyrazolo[3,4-d]-pyrimidinon-derivate |
| HUP0301112A3 (en) | 2000-02-18 | 2005-04-28 | Shire Biochem Inc Laval | Method for the treatment or prevention of flavivirus infections using nucleoside analogues |
| CN1471397A (zh) * | 2000-08-30 | 2004-01-28 | 利利艾科斯有限公司 | 治疗偏头痛的方法 |
| RS50236B (sr) | 2001-01-22 | 2009-07-15 | Merck & Co.Inc., | Nukleozidni derivati kao inhibitori rnk-zavisne rnk virusne polimeraze |
| WO2004009921A2 (en) | 2002-07-19 | 2004-01-29 | Mossor David B | Portable shielding system |
| 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 |
| DE10238722A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse |
| 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 |
| JP2006525966A (ja) * | 2003-05-09 | 2006-11-16 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | ６−シクリルメチル−および６−アルキルメチル置換ピラゾロピリミジン類 |
| 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 |
| CA2596424C (en) | 2005-02-04 | 2016-03-29 | Millennium Pharmaceuticals, Inc. | Inhibitors of e1 activating enzymes |
| GEP20125405B (en) * | 2007-05-11 | 2012-02-27 | Pfizer | Amino-heterocyclic compounds |
| CA2706018C (en) | 2007-11-30 | 2015-11-24 | Boehringer Ingelheim International Gmbh | 1, 5-dihydro-pyrazolo [3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators 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 |
| NZ590788A (en) * | 2008-09-08 | 2012-11-30 | Boehringer Ingelheim Int | Pyrazolopyrimidines and their use for the treatment of cns disorders |
| CA2757231A1 (en) | 2009-03-31 | 2010-10-07 | Boehringer Ingelheim International Gmbh | 1-heterocyclyl-1,5-dihydro-pyrazolo [3,4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| AR077859A1 (es) * | 2009-08-12 | 2011-09-28 | Boehringer Ingelheim Int | Compuestos para el tratamiento de trastornos del snc |
| GEP20156217B (en) * | 2010-08-12 | 2015-01-12 | Boehringer Ingelheim Int | 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors |
-
2012
- 2012-02-09 US US13/369,623 patent/US20130040971A1/en not_active Abandoned
- 2012-02-13 AP AP2013007045A patent/AP2013007045A0/xx unknown
- 2012-02-13 PE PE2013001871A patent/PE20140970A1/es not_active Application Discontinuation
- 2012-02-13 SG SG2013061494A patent/SG192756A1/en unknown
- 2012-02-13 WO PCT/EP2012/052378 patent/WO2012110440A1/en not_active Ceased
- 2012-02-13 JP JP2013552980A patent/JP2014505091A/ja active Pending
- 2012-02-13 CA CA2827261A patent/CA2827261A1/en not_active Abandoned
- 2012-02-13 AR ARP120100472A patent/AR085219A1/es unknown
- 2012-02-13 TW TW101104596A patent/TW201245199A/zh unknown
- 2012-02-13 MX MX2013009343A patent/MX2013009343A/es active IP Right Grant
- 2012-02-13 EP EP20120705246 patent/EP2675807B1/en active Active
- 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 CN CN2012800177072A patent/CN103459397A/zh active Pending
- 2012-02-13 EA EA201300908A patent/EA023574B1/ru not_active IP Right Cessation
- 2012-02-13 MA MA36160A patent/MA34889B1/fr unknown
- 2012-02-13 KR KR1020137021400A patent/KR20140010036A/ko not_active Withdrawn
- 2012-02-13 PH PH1/2013/501677A patent/PH12013501677A1/en unknown
-
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 |
|---|---|
| US20130040971A1 (en) | 2013-02-14 |
| KR20140010036A (ko) | 2014-01-23 |
| TN2013000324A1 (en) | 2015-01-20 |
| MA34889B1 (fr) | 2014-02-01 |
| WO2012110440A1 (en) | 2012-08-23 |
| CL2013002341A1 (es) | 2014-04-04 |
| AR085219A1 (es) | 2013-09-18 |
| MX2013009343A (es) | 2013-10-01 |
| BR112013020605A2 (pt) | 2016-10-18 |
| PE20140970A1 (es) | 2014-08-03 |
| EP2675807B1 (en) | 2015-04-22 |
| AP2013007045A0 (en) | 2013-08-31 |
| CA2827261A1 (en) | 2012-08-23 |
| IL227526A0 (en) | 2013-09-30 |
| PH12013501677A1 (en) | 2018-04-11 |
| AU2012217208A1 (en) | 2013-08-01 |
| CO6791616A2 (es) | 2013-11-14 |
| TW201245199A (en) | 2012-11-16 |
| ECSP13012852A (es) | 2014-09-30 |
| WO2012110440A9 (en) | 2013-03-14 |
| EP2675807A1 (en) | 2013-12-25 |
| SG192756A1 (en) | 2013-09-30 |
| CN103459397A (zh) | 2013-12-18 |
| JP2014505091A (ja) | 2014-02-27 |
| EA023574B1 (ru) | 2016-06-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA201300908A1 (ru) | ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9A | |
| EA201201664A1 (ru) | Производные 6-циклоалкил-1,5-дигидропипазоло[3,4-d]пиримидин-4-она и их применение в качестве ингибиторов pde9a | |
| EA201101395A1 (ru) | Производные 1-гетероциклил-1,5-дигидропиразоло[3,4d]пиримидин-4-oha и их применение в качестве модуляторов pde9a | |
| EA201590870A1 (ru) | АМИНОЗАМЕЩЕННЫЕ ИМИДАЗО[1,2-a]ПИРИДИНКАРБОКСАМИДЫ И ИХ ПРИМЕНЕНИЕ | |
| CA2918938C (en) | Substituted aminopyrimidine compounds and methods of use | |
| EA201201191A1 (ru) | 4-[циклоалкилокси(гетеро)ариламино]тиено[2,3-d]пиримидины, обладающие ингибирующей активностью по отношению к mnkl/mnk2, предназначенные для фармацевтических композиций | |
| BR112015025140A2 (pt) | 2-fenilimidazo[1,2-a]pirimidinas como agentes de imagem | |
| EA201200952A1 (ru) | Производные пиразина и их применение для лечения неврологических нарушений | |
| BR112015016315A2 (pt) | fluoro-[1,3]oxazinas como inibidores de bace1 | |
| GEP201706780B (en) | Substituted 2-aza-bicyclo [2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c | |
| BR112015003592A2 (pt) | derivados de 1,6-diazabiciclo[3,2,1]octan-7-ona e seu uso no tratamento de infecções bacterianas | |
| EA201590663A1 (ru) | ПРОИЗВОДНЫЕ ПИРРОЛО[3,2-d]ПИРИМИДИНА ДЛЯ ЛЕЧЕНИЯ ВИРУСНЫХ ИНФЕКЦИЙ И ДРУГИХ ЗАБОЛЕВАНИЙ | |
| EA201391786A1 (ru) | Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и/или bace2 | |
| BR112015024678A2 (pt) | inibidor da cinase | |
| EA201201192A1 (ru) | Тиенопиримидины, содержащие замещенную алкильную группу, предназначенные для фармацевтических композиций | |
| EA201490540A1 (ru) | Соединения и композиции в качестве ингибиторов с-kit киназы | |
| BR112013032974A2 (pt) | "derivados de 1,6-diazabiciclo [3,2,1]-octan-7-ona, seus usos, e composições farmacêuticas". | |
| EA201391670A1 (ru) | 1,3-оксазины в качестве ингибиторов bace1 и/или bace2 | |
| EA201300556A1 (ru) | Аминоспиртзамещенные производные 2,3-дигидроимидазо[1,2-с] хиназолина, пригодные для лечения гиперпролиферативных нарушений и заболеваний, связанных с ангиогенезом | |
| EA202090258A2 (ru) | ПРОИЗВОДНЫЕ ПИРРОЛО[3,2-d]ПИРИМИДИНА ДЛЯ ЛЕЧЕНИЯ ВИРУСНЫХ ИНФЕКЦИЙ И ДРУГИХ ЗАБОЛЕВАНИЙ | |
| WO2014033447A3 (en) | Diaryl urea derivatives as p38 map kinase inhibitors | |
| WO2015095337A3 (en) | PYRAZOLO[1,5-a]PYRIMIDINECARBOXAMIDE DERIVATIVES FOR TREATING COGNITIVE IMPAIRMENT | |
| UA113186C2 (xx) | Макроциклічні інгібітори lrrk2 кінази | |
| UA107952C2 (ru) | Производные имидазо [1,2-a] пиразина и их применение для профилактики или лечения неврологических, психиатрических и метаболических расстройств и заболеваний | |
| EA201591379A1 (ru) | Липопротеин-ассоциированные ингибиторы фосфолипазы a2 (lp-pla) на основе 2,3-дигидроимидазо[1,2-с]пиримидин-5(1h)-онов |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |