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)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Psychiatry (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) | US8450331B2 (es) |
| EP (2) | EP2283016B1 (es) |
| JP (2) | JP2011518225A (es) |
| KR (1) | KR20110003347A (es) |
| CN (1) | CN102066380A (es) |
| AR (2) | AR072952A1 (es) |
| AU (2) | AU2009239535A1 (es) |
| BR (1) | BRPI0911356A2 (es) |
| CA (2) | CA2723222C (es) |
| CL (2) | CL2009000953A1 (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) | TW200948364A (es) |
| WO (2) | WO2009131974A1 (es) |
| ZA (1) | ZA201007433B (es) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| JP2008543849A (ja) | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | アスパルチルプロテアーゼ阻害剤 |
| BRPI0612545A2 (pt) | 2005-06-14 | 2010-11-23 | Schering Corp | compostos inibidores de protease, composições farmacêuticas e uso dos mesmos |
| AU2006307314C1 (en) | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| CA2651519A1 (en) | 2006-06-06 | 2007-12-13 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CA2653650A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| 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 |
| JP5701608B2 (ja) | 2007-12-06 | 2015-04-15 | 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 |
| MX2010011563A (es) | 2008-04-22 | 2010-11-12 | Schering Corp | Compuestos 2-imino-3-metil pirrolo pirimidinona fenil-sustituidos como inhibidores de enzima de escision de proteina precursora amiloide sitio beta-1, composiciones y su uso. |
| EA020740B1 (ru) | 2008-06-13 | 2015-01-30 | Шионоги & Ко., Лтд. | Серосодержащее гетероциклическое производное, обладающее активностью ингибитора бета-секретазы |
| CN102209721A (zh) | 2008-09-11 | 2011-10-05 | 安姆根有限公司 | 作为β-分泌酶调节剂的螺四环化合物及其使用方法 |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| GEP20146046B (en) | 2008-12-06 | 2014-02-25 | Intracellular Therapies Inc | Organic compounds |
| PE20110834A1 (es) | 2008-12-06 | 2011-12-14 | Intra Cellular Therapies Inc | DERIVADOS DE PIRROL[3,4-d]PIRIMIDINA COMO INHIBIDORES DE FOSFODIESTERASA 1 (PDE1) |
| BRPI0922700A2 (pt) | 2008-12-06 | 2015-08-11 | Intracellular Therapies Inc | Compostos orgânicos |
| US8557826B2 (en) | 2009-10-08 | 2013-10-15 | Merck Sharp & Dohme Corp. | 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 | |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| US20120245155A1 (en) | 2009-12-11 | 2012-09-27 | Shionogi & Co., Ltd. | Fused heterocyclic compound having amino group |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| MX2012010658A (es) | 2010-03-15 | 2012-12-05 | Amgen Inc | Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa. |
| EP2547686B1 (en) | 2010-03-15 | 2014-01-22 | Amgen Inc. | Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use |
| EP2575817A4 (en) | 2010-05-31 | 2014-01-08 | Intra Cellular Therapies Inc | ORGANIC CONNECTIONS |
| EP2590657A4 (en) * | 2010-05-31 | 2014-02-12 | Intra Cellular Therapies Inc | ORGANIC CONNECTIONS |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| AU2011321427A1 (en) | 2010-10-29 | 2013-05-02 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
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| 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 |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| CA2832473A1 (en) | 2011-04-13 | 2012-10-18 | Merck Sharp & Dohme Corp. | 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions, and their use |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
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| US8865723B2 (en) | 2012-10-25 | 2014-10-21 | Tetra Discovery Partners Llc | Selective PDE4 B inhibition and improvement in cognition in subjects with brain injury |
| ES2616835T3 (es) * | 2012-10-26 | 2017-06-14 | Eli Lilly And Company | Derivados de tetrahidropirrolotiazina como inhibidores de bace |
| WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| WO2014099788A1 (en) * | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| 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 |
| PT2017095250B (pt) | 2015-11-30 | 2021-08-06 | Univ De Coimbra | Peptídeos inibidores da bace1 para o tratamento de doenças neurológicas |
| PE20210447A1 (es) * | 2018-02-28 | 2021-03-08 | Japan Tobacco Inc | Compuestos de dihidropirimidinona o dihidrotriazinona fusionados con anillos saturados y su uso farmaceutico |
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- 2009-04-21 TW TW098113220A patent/TW200948364A/zh unknown
- 2009-04-21 CN CN200980124480XA patent/CN102066380A/zh active Pending
- 2009-04-21 CL CL2009000953A patent/CL2009000953A1/es unknown
- 2009-04-21 JP JP2011506387A patent/JP2011518225A/ja not_active Ceased
- 2009-04-21 TW TW098113228A patent/TW201004957A/zh unknown
- 2009-04-21 AR ARP090101393A patent/AR072952A1/es not_active Application Discontinuation
- 2009-04-21 BR BRPI0911356A patent/BRPI0911356A2/pt not_active IP Right Cessation
- 2009-04-21 EP EP09734309.9A patent/EP2283016B1/en not_active Not-in-force
- 2009-04-21 AU AU2009239535A patent/AU2009239535A1/en not_active Abandoned
- 2009-04-21 CL CL2009000954A patent/CL2009000954A1/es unknown
- 2009-04-21 KR KR1020107023569A patent/KR20110003347A/ko not_active Ceased
- 2009-04-21 EP EP09734237.2A patent/EP2288613B1/en active Active
- 2009-04-21 CA CA2723222A patent/CA2723222C/en not_active Expired - Fee Related
- 2009-04-21 WO PCT/US2009/041201 patent/WO2009131974A1/en not_active Ceased
- 2009-04-21 PE PE2009000554A patent/PE20091734A1/es not_active Application Discontinuation
- 2009-04-21 US US12/988,464 patent/US8450331B2/en active Active
- 2009-04-21 JP JP2011506386A patent/JP2011518224A/ja not_active Withdrawn
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