PE20181447A1 - Derivados de eter ciclico de pirazolo[1,5-a]pirimidin-3-carboxiamida - Google Patents
Derivados de eter ciclico de pirazolo[1,5-a]pirimidin-3-carboxiamidaInfo
- Publication number
- PE20181447A1 PE20181447A1 PE2018001274A PE2018001274A PE20181447A1 PE 20181447 A1 PE20181447 A1 PE 20181447A1 PE 2018001274 A PE2018001274 A PE 2018001274A PE 2018001274 A PE2018001274 A PE 2018001274A PE 20181447 A1 PE20181447 A1 PE 20181447A1
- Authority
- PE
- Peru
- Prior art keywords
- halogen
- optionally substituted
- pyrazolo
- cyclic ether
- substituents
- Prior art date
Links
- 150000004292 cyclic ethers Chemical class 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 101001098814 Dictyostelium discoideum 3',5'-cyclic-nucleotide phosphodiesterase regA Proteins 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- -1 cyclic ether derivatives of pyrazolo [1,5-a] pyrimidine-3-carboxyamide Chemical class 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
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- 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
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- 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
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- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- 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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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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
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- A61P3/04—Anorexiants; Antiobesity agents
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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
- A61P3/06—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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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
- A61P9/00—Drugs for disorders of the cardiovascular system
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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
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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
- C07D307/22—Nitrogen atoms not forming part of a nitro radical
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Virology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Reproductive Health (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Anesthesiology (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
Abstract
Referido a un compuesto de formula (I), en donde A se selecciona del grupo (Aa); R1 es halogeno, C1-3-alquil- y C3-6-cicloalquil-, los cuales se pueden sustituir opcionalmente con 1 a 5 sustituyentes seleccionados independientemente entre halogeno, NC- y HO-; R2 es arilo o heteroarilo; R3 es H o C1-3-alquil, los cuales pueden se pueden sustituir opcionalmente con 1 a 7 sustituyentes seleccionados independientemente entre si; R5 es H-, halogeno, NC- entre otros, se pueden sustituir opcionalmente con 1 a 5 sustituyentes, seleccionados independientemente entre HO- y F-; R6 es H-, halogeno, entre otros, se pueden sustituir opcionalmente con 1 a 5 sustituyentes seleccionados independientemente entre HO- y F-. Estos compuestos son derivados de eter ciclico de pirazolo[1,5-a]pirimidin-3-carboxiamida, inhibidores de la fosfodiesterasa 2, utiles en el tratamiento de enfermedades del sistema nervioso central y otras enfermedades. Ademas, se refiere a procesos para preparar composiciones farmaceuticas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15189600.8A EP3156405A1 (en) | 2015-10-13 | 2015-10-13 | Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181447A1 true PE20181447A1 (es) | 2018-09-12 |
Family
ID=54293164
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018001274A PE20181447A1 (es) | 2015-10-13 | 2016-10-12 | Derivados de eter ciclico de pirazolo[1,5-a]pirimidin-3-carboxiamida |
| PE2018000540A PE20190778A1 (es) | 2015-10-13 | 2016-10-12 | Derivados de eter ciclico de pirazolo[1,5-a]pirimidin-3-carboxiamida |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018000540A PE20190778A1 (es) | 2015-10-13 | 2016-10-12 | Derivados de eter ciclico de pirazolo[1,5-a]pirimidin-3-carboxiamida |
Country Status (30)
| Country | Link |
|---|---|
| US (5) | US10023575B2 (es) |
| EP (2) | EP3156405A1 (es) |
| JP (1) | JP6626965B2 (es) |
| KR (1) | KR102611558B1 (es) |
| CN (2) | CN108137602B (es) |
| AU (1) | AU2016338602B2 (es) |
| BR (1) | BR112018004347B1 (es) |
| CA (1) | CA3001929C (es) |
| CL (1) | CL2018000856A1 (es) |
| CO (1) | CO2018003756A2 (es) |
| CY (1) | CY1125323T1 (es) |
| DK (1) | DK3362453T3 (es) |
| EA (1) | EA035350B1 (es) |
| ES (1) | ES2912223T3 (es) |
| HR (1) | HRP20220595T1 (es) |
| IL (1) | IL258070B (es) |
| LT (1) | LT3362453T (es) |
| MA (1) | MA42988B1 (es) |
| MX (1) | MX376458B (es) |
| MY (1) | MY195169A (es) |
| NZ (1) | NZ740119A (es) |
| PE (2) | PE20181447A1 (es) |
| PH (1) | PH12018500796B1 (es) |
| PL (1) | PL3362453T3 (es) |
| PT (1) | PT3362453T (es) |
| RS (1) | RS63218B1 (es) |
| SA (1) | SA518391334B1 (es) |
| SI (1) | SI3362453T1 (es) |
| UA (1) | UA124576C2 (es) |
| WO (1) | WO2017064082A1 (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3156405A1 (en) | 2015-10-13 | 2017-04-19 | Boehringer Ingelheim International GmbH | Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide |
| RU2671964C1 (ru) * | 2017-08-30 | 2018-11-08 | Сиа Эволед | Пиразоло[1,5-а]пиримидинкарбоксилаты гадолиния и органические светодиоды на их основе |
| US11498928B2 (en) | 2019-01-18 | 2022-11-15 | Ascentage Pharma (Suzhou) Co., Ltd. | Macrocyclic spiroethers as Mcl-1 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 |
| EP4045037A4 (en) * | 2019-10-16 | 2023-11-15 | ChemoCentryx, Inc. | HETEROARYL-BIPHENYL AMINE FOR THE TREATMENT OF PD-L1 DISEASE |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10108752A1 (de) | 2001-02-23 | 2002-09-05 | Bayer Ag | Neue Substituierte Imidazotriazinone |
| PL382706A1 (pl) * | 2002-08-26 | 2007-11-26 | Takeda Pharmaceutical Company Limited | Związek modulujący receptor wapnia i jego zastosowanie |
| WO2004024728A2 (en) | 2002-09-16 | 2004-03-25 | Glaxo Group Limited | Pyrazolo[3,4-b]pyridine compounds, and their use as phosphodiesterase inhibitors |
| WO2005041957A1 (en) | 2003-10-29 | 2005-05-12 | Pfizer Products Inc. | Oxindole derivatives and their use as phosphodiesterase type 2 inhibitors |
| AU2004303609A1 (en) | 2003-12-16 | 2005-07-07 | Pfizer Products Inc. | Pyrido[2,3-d]pyrimidine-2,4-diamines as PDE 2 inhibitors |
| EP1548011A1 (en) | 2003-12-23 | 2005-06-29 | Neuro3D | Benzo[1,4]diazepin-2-one derivatives as phosphodiesterase PDE2 inhibitors, preparation and therapeutic use thereof |
| JP2007528400A (ja) | 2004-03-09 | 2007-10-11 | エラン ファーマシューティカルズ，インコーポレイテッド | 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 |
| FR2870539B1 (fr) | 2004-05-19 | 2006-08-04 | Greenpharma Sa Sa | Nouvelles methodes et medicaments |
| AU2005279221C9 (en) | 2004-09-02 | 2012-08-23 | Takeda Gmbh | Triazolophthalazines |
| WO2006072615A2 (en) | 2005-01-05 | 2006-07-13 | Nycomed Gmbh | Triazolophthalazines as pde2-inhibitors |
| CA2591991C (en) | 2005-01-05 | 2013-11-19 | Altana Pharma Ag | Triazolophthalazines |
| BRPI0502411A (pt) | 2005-03-31 | 2006-11-28 | Univ Minas Gerais | processo de desenvolvimento de substáncias como inibidores potentes e seletivos de isoformas de fosfodiesterases dos tipos 1 a 5 (pde1,pde2,pde3, pde4, pde5) na base de diocleìna, fluranol ou análogos e suas composições farmacêuticas para o estudo e tratamento de doenças cardiovasculares e produtos associados |
| WO2007046548A1 (en) * | 2005-10-21 | 2007-04-26 | Mitsubishi Tanabe Pharma Corporation | Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists |
| JP4847275B2 (ja) * | 2005-10-21 | 2011-12-28 | 田辺三菱製薬株式会社 | ピラゾロ［１，５−ａ］ピリミジン化合物 |
| TWI372760B (en) * | 2005-10-21 | 2012-09-21 | Mitsubishi Tanabe Pharma Corp | A pyrazolo[1,5-a]pyrimidine compound |
| WO2007121319A2 (en) | 2006-04-14 | 2007-10-25 | University Of California | Compostions and methods for determining and predicting treatment responses for depression and anxiety |
| AR061793A1 (es) * | 2006-07-05 | 2008-09-24 | Mitsubishi Tanabe Pharma Corp | Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica |
| TWI419889B (zh) * | 2006-07-05 | 2013-12-21 | Mitsubishi Tanabe Pharma Corp | 吡唑并〔１，５-ａ〕嘧啶化合物 |
| JPWO2008026687A1 (ja) | 2006-09-01 | 2010-01-21 | 杏林製薬株式会社 | ピラゾロピリジンカルボキサミド誘導体及びそれらを含有するホスホジエステラーゼ（ｐｄｅ）阻害剤 |
| DE102006048693A1 (de) | 2006-10-14 | 2008-04-17 | Bayer Healthcare Ag | Inhibition der PDE2A |
| GB0813144D0 (en) | 2008-07-17 | 2008-08-27 | Glaxo Group Ltd | Novel compounds |
| WO2010051549A1 (en) * | 2008-10-31 | 2010-05-06 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
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