ECSP10010585A - Compuestos de 2- imido- 3- metil pirrolo pirimidinona fenilo- sustituidos como inhibidores bace- 1, composiciones, y su uso - Google Patents
Compuestos de 2- imido- 3- metil pirrolo pirimidinona fenilo- sustituidos como inhibidores bace- 1, composiciones, y su usoInfo
- Publication number
- ECSP10010585A ECSP10010585A EC2010010585A ECSP10010585A ECSP10010585A EC SP10010585 A ECSP10010585 A EC SP10010585A EC 2010010585 A EC2010010585 A EC 2010010585A EC SP10010585 A ECSP10010585 A EC SP10010585A EC SP10010585 A ECSP10010585 A EC SP10010585A
- Authority
- EC
- Ecuador
- Prior art keywords
- compounds
- methyl
- pirroid
- bace
- pyrimidinone
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- YCIPQJTZJGUXND-UHFFFAOYSA-N Aglaia odorata Alkaloid Natural products C1=CC(OC)=CC=C1C1(C(C=2C(=O)N3CCCC3=NC=22)C=3C=CC=CC=3)C2(O)C2=C(OC)C=C(OC)C=C2O1 YCIPQJTZJGUXND-UHFFFAOYSA-N 0.000 title 1
- 229940125759 BACE1 protease inhibitor Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical compound OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 title 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate 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
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P25/14—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
- A61P25/28—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
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
En una realización, el presente invento proporciona ciertos compuestos de 2- imino- 3- metil pirrolo pirimidona (colectivamente o individualmente citados en la presente como "compuestos del invento") , como se describieron en la presente.En una realización, los compuestos del invento tienen la fórmula estructural (II): e incluyen tautómeros del mismo, y sales farmacéuticamente aceptables y solvatos de dichos compuestos y dichos tautómeros, en donde R2, R3, R4, R5, R6, R7, R8, y R9 son cada uno son seleccionados independientemente así definidos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4700608P | 2008-04-22 | 2008-04-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP10010585A true ECSP10010585A (es) | 2011-04-29 |
Family
ID=40806727
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2010010585A ECSP10010585A (es) | 2008-04-22 | 2010-10-29 | Compuestos de 2- imido- 3- metil pirrolo pirimidinona fenilo- sustituidos como inhibidores bace- 1, composiciones, y su uso |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8541427B2 (es) |
| EP (2) | EP2288613B1 (es) |
| JP (2) | JP2011518225A (es) |
| KR (1) | KR20110003347A (es) |
| CN (1) | CN102066380A (es) |
| AR (2) | AR071385A1 (es) |
| AU (2) | AU2009239536C1 (es) |
| BR (1) | BRPI0911356A2 (es) |
| CA (2) | CA2723222C (es) |
| CL (2) | CL2009000954A1 (es) |
| CO (1) | CO6321265A2 (es) |
| CR (1) | CR11738A (es) |
| DO (1) | DOP2010000320A (es) |
| EA (1) | EA201001532A1 (es) |
| EC (1) | ECSP10010585A (es) |
| IL (1) | IL208465A0 (es) |
| MA (1) | MA32252B1 (es) |
| MX (1) | MX2010011563A (es) |
| PE (2) | PE20091734A1 (es) |
| SV (1) | SV2010003714A (es) |
| TW (2) | TW201004957A (es) |
| WO (2) | WO2009131974A1 (es) |
| ZA (1) | ZA201007433B (es) |
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| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) * | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| WO2006138264A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| US8722708B2 (en) | 2005-06-14 | 2014-05-13 | Merck Sharp & Dohme Inc. | Substituted isoindolines as aspartyl protease inhibitors |
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| AU2007256633B2 (en) | 2006-06-06 | 2013-09-12 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CA2653650A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
| ES2588238T3 (es) | 2007-12-06 | 2016-10-31 | Intra-Cellular Therapies, Inc. | Derivados de pirazolopirimidin-4,6-diona y su uso como producto farmacéutico |
| AU2009239536C1 (en) * | 2008-04-22 | 2012-12-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| MX2011002705A (es) | 2008-09-11 | 2011-09-09 | Amgen Inc | Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso. |
| 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 |
| BRPI0922700A2 (pt) | 2008-12-06 | 2015-08-11 | Intracellular Therapies Inc | Compostos orgânicos |
| MX2011005934A (es) | 2008-12-06 | 2011-12-16 | Intra Cellular Therapies Inc | Compuestos organicos. |
| AU2009322899A1 (en) | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2011044185A2 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| US20120245155A1 (en) | 2009-12-11 | 2012-09-27 | Shionogi & Co., Ltd. | Fused heterocyclic compound having amino group |
| MX2012010658A (es) | 2010-03-15 | 2012-12-05 | Amgen Inc | Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa. |
| US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EP2575817A4 (en) | 2010-05-31 | 2014-01-08 | Intra Cellular Therapies Inc | ORGANIC CONNECTIONS |
| US9371327B2 (en) | 2010-05-31 | 2016-06-21 | Intra-Cellular Therapies, Inc. | PDE1 inhibitor compounds |
| CA2816285A1 (en) | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
| GB201100181D0 (en) * | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| EP2694521B1 (en) * | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2012138734A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| BR112013026341A2 (pt) | 2011-04-13 | 2019-09-24 | Merck Sharp & Dohe Corp. | composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia |
| 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 |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
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| CA2886507C (en) * | 2012-10-26 | 2016-09-20 | Eli Lilly And Company | Bace inhibitors |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9580396B2 (en) | 2012-12-21 | 2017-02-28 | Merck Sharp & Dohme Corp. | C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use |
| TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
| CN103910781B (zh) * | 2014-03-18 | 2016-02-17 | 重庆大学 | 一种Aβ聚集抑制剂 |
| US9546175B2 (en) | 2014-08-07 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN104761557B (zh) * | 2015-04-08 | 2017-02-22 | 河南师范大学 | 六氢‑1H‑吡咯并[3,4‑d]嘧啶类化合物及其制备方法 |
| WO2017095250A1 (en) | 2015-11-30 | 2017-06-08 | Centro De Neurociências E Biologia Celular | Peptide inhibitors of bace1 for the treatment of neurological disorders |
| CN111741948B (zh) * | 2018-02-28 | 2023-11-10 | 日本烟草产业株式会社 | 饱和环稠合的二氢嘧啶酮或二氢三嗪酮化合物及其药物用途 |
| CN109503582A (zh) * | 2018-12-17 | 2019-03-22 | 上海合全药物研发有限公司 | 顺式螺[哌啶并-4,1'-吡咯并[3,4-c]吡咯]-1-甲酸叔丁酯的合成方法 |
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- 2009-04-21 AU AU2009239536A patent/AU2009239536C1/en not_active Ceased
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- 2009-04-21 BR BRPI0911356A patent/BRPI0911356A2/pt not_active IP Right Cessation
- 2009-04-21 AR ARP090101392A patent/AR071385A1/es not_active Application Discontinuation
- 2009-04-21 JP JP2011506387A patent/JP2011518225A/ja not_active Ceased
- 2009-04-21 JP JP2011506386A patent/JP2011518224A/ja not_active Withdrawn
- 2009-04-21 WO PCT/US2009/041201 patent/WO2009131974A1/en not_active Ceased
- 2009-04-21 WO PCT/US2009/041202 patent/WO2009131975A1/en not_active Ceased
- 2009-04-21 EA EA201001532A patent/EA201001532A1/ru unknown
- 2009-04-21 KR KR1020107023569A patent/KR20110003347A/ko not_active Ceased
- 2009-04-21 MX MX2010011563A patent/MX2010011563A/es not_active Application Discontinuation
- 2009-04-21 AR ARP090101393A patent/AR072952A1/es not_active Application Discontinuation
- 2009-04-21 TW TW098113228A patent/TW201004957A/zh unknown
- 2009-04-21 US US12/988,461 patent/US8541427B2/en active Active
- 2009-04-21 PE PE2009000554A patent/PE20091734A1/es not_active Application Discontinuation
- 2009-04-21 CL CL2009000954A patent/CL2009000954A1/es unknown
- 2009-04-21 CA CA2721738A patent/CA2721738A1/en not_active Abandoned
- 2009-04-21 PE PE2009000553A patent/PE20091834A1/es not_active Application Discontinuation
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- 2009-04-21 EP EP09734237.2A patent/EP2288613B1/en active Active
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- 2009-04-21 CN CN200980124480XA patent/CN102066380A/zh active Pending
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