BRPI0618845A2 - composto, formulação farmacêutica, uso de um composto, e, métodos para a inibição da atividade de bace e para o tratamento ou a prevenção de uma patologia relacionada a abeta em um mamífero - Google Patents

composto, formulação farmacêutica, uso de um composto, e, métodos para a inibição da atividade de bace e para o tratamento ou a prevenção de uma patologia relacionada a abeta em um mamífero

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Publication number
BRPI0618845A2
BRPI0618845A2 BRPI0618845A BRPI0618845A BRPI0618845A2 BR PI0618845 A2 BRPI0618845 A2 BR PI0618845A2 BR PI0618845 A BRPI0618845 A BR PI0618845A BR PI0618845 A BRPI0618845 A BR PI0618845A BR PI0618845 A2 BRPI0618845 A2 BR PI0618845A2
Authority
BR
Brazil
Prior art keywords
compound
fir
mammal
treating
preventing
Prior art date
Application number
BRPI0618845A
Other languages
English (en)
Inventor
Christopher Murray
Gianni Chessari
Jacob Kihlström
Jeremy Burrows
Johan Hedström
Johan Lindström
Karin Kolmodin
Katarina Högdin
Miles Stuart Congreve
Sahil Patel
Stefan Berg
Sven Hellberg
Original Assignee
Astex Therapeutics Ltd
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38049092&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0618845(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astex Therapeutics Ltd, Astrazeneca Ab filed Critical Astex Therapeutics Ltd
Publication of BRPI0618845A2 publication Critical patent/BRPI0618845A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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    • 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
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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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    • 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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    • 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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    • C07C25/00—Compounds containing at least one halogen atom bound to a six-membered aromatic ring
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    • C07C43/174—Unsaturated ethers containing halogen containing six-membered aromatic rings
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    • C07C47/00—Compounds having —CHO groups
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    • C07C49/782—Ketones containing a keto group bound to a six-membered aromatic ring polycyclic
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    • C07C49/80—Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
    • C07C49/813—Ketones containing a keto group bound to a six-membered aromatic ring containing halogen polycyclic
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    • C07C49/82—Ketones containing a keto group bound to a six-membered aromatic ring containing hydroxy groups
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    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
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    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/06—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
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    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
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    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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  • Chemical & Material Sciences (AREA)
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  • Heart & Thoracic Surgery (AREA)
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  • Urology & Nephrology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
BRPI0618845A 2005-11-21 2006-11-20 composto, formulação farmacêutica, uso de um composto, e, métodos para a inibição da atividade de bace e para o tratamento ou a prevenção de uma patologia relacionada a abeta em um mamífero BRPI0618845A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US73865005P 2005-11-21 2005-11-21
US81574606P 2006-06-22 2006-06-22
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Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
SG162790A1 (en) 2005-06-14 2010-07-29 Schering Corp Aspartyl protease inhibitors
CN103936690B (zh) 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
WO2007058601A1 (en) * 2005-11-21 2007-05-24 Astrazeneca Ab Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
WO2008076044A1 (en) * 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5, 5-diaryl-imidazol-4-ones
TW200831091A (en) * 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
US8168630B2 (en) 2007-04-24 2012-05-01 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
TW200902503A (en) * 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
MX2010008347A (es) * 2008-02-18 2010-11-12 Hoffmann La Roche Derivados de 4,5-dihidro-oxazol-2-ilamina.
MX2010013256A (es) 2008-06-13 2010-12-21 Shionogi & Co Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa.
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
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
JP5381257B2 (ja) * 2009-04-09 2014-01-08 ユニマテック株式会社 含フッ素ボロン酸エステル化合物の製造方法
TW201103893A (en) * 2009-07-02 2011-02-01 Astrazeneca Ab New compounds
AR077447A1 (es) * 2009-07-02 2011-08-31 Astrazeneca Ab Compuestos inhibidores de beta-secretasa, utiles para el tratamiento de enfermedades neurodegenerativas
CN102030770B (zh) * 2009-09-25 2012-10-31 北京大学 一种芳香硼酸酯化合物的制备方法
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011071135A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
EP2368884A1 (en) 2010-03-25 2011-09-28 Laboratorios Lesvi, S.L. Process for the preparation of bosentan
RS60310B1 (sr) 2010-08-10 2020-07-31 Rempex Pharmaceuticals Inc Ciklični derivati estra boronske kiseline, postupak za pripremu injihove terapeutske upotrebe
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
EP2634186A4 (en) 2010-10-29 2014-03-26 Shionogi & Co naphthyridine
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
EP2673279A1 (en) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
US8962859B2 (en) 2011-02-15 2015-02-24 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
MX2014002113A (es) 2011-08-22 2014-04-25 Merck Sharp & Dohme Iminotiazinas sustituidas en 2-espiro y sus mono y bioxidos como inhibidores de enzima de disociacion de proteina precursora amiloide del sitio beta, composiciones, y su uso.
US9012491B2 (en) 2011-08-31 2015-04-21 Rempex Pharmaceuticals, Inc. Heterocyclic boronic acid ester derivatives and therapeutic uses thereof
US9296759B2 (en) 2011-09-21 2016-03-29 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
JP5853617B2 (ja) * 2011-11-11 2016-02-09 Dic株式会社 アゾベンゼン誘導体及びこれを含有する液晶組成物
US9156858B2 (en) 2012-05-23 2015-10-13 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US10561675B2 (en) 2012-06-06 2020-02-18 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
US10548882B2 (en) * 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt
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
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9241947B2 (en) 2013-01-04 2016-01-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
CA2894891A1 (en) 2013-01-04 2014-07-10 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US9101638B2 (en) 2013-01-04 2015-08-11 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EA201591004A1 (ru) 2013-01-04 2016-02-29 Ремпекс Фармасьютикалз, Инк. Производные бороновой кислоты и их терапевтическое применение
US9353089B2 (en) 2013-03-26 2016-05-31 Saint Louis University Compositions and methods for the treatment of malaria
BR112015026261A8 (pt) 2013-04-16 2017-12-26 Actelion Pharmaceuticals Ltd Derivados biaromáticos antibacterianos
WO2015171398A1 (en) 2014-05-05 2015-11-12 Rempex Pharmaceuticals, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
US10385074B2 (en) 2014-05-05 2019-08-20 Rempex Pharmaceuticals, Inc. Synthesis of boronate salts and uses thereof
CA2947041A1 (en) 2014-05-19 2015-11-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EA201692301A1 (ru) 2014-07-01 2017-06-30 Ремпекс Фармасьютикалз, Инк. Производные бороновой кислоты и их терапевтическое применение
WO2016081297A1 (en) 2014-11-18 2016-05-26 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
US20180051041A1 (en) 2015-03-17 2018-02-22 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
MY196909A (en) 2016-06-30 2023-05-09 Qpex Biopharma Inc Boronic acid derivatives and therapeutic uses thereof
CA3078627A1 (en) 2017-10-11 2019-04-18 Qpex Biopharma, Inc. Boronic acid derivatives and synthesis thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1699455T1 (sl) * 2003-12-15 2013-10-30 Merck Sharp & Dohme Corp. Heterocikliäśni aspartil proteazni inhibitorji
US7700603B2 (en) * 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
CN1968945A (zh) * 2004-06-16 2007-05-23 惠氏公司 用于抑制β分泌酶的氨基－5,5－二苯基咪唑酮衍生物
EP1891021B1 (en) * 2005-06-14 2019-01-23 Merck Sharp & Dohme Corp. Aspartyl protease inhibitors
AR053902A1 (es) * 2005-06-14 2007-05-23 Schering Corp Inhibidores de aspartil proteasa heterociclicos macrociclicos
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
CA2613435A1 (en) * 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for .beta.-secretase modulation
PE20070531A1 (es) * 2005-10-27 2007-07-13 Schering Corp Compuestos heterociclicos como inhibidores de aspartil proteasas
AR056211A1 (es) * 2005-10-31 2007-09-26 Schering Corp Derivados de [1,4,6]oxadiazepinas, composiciones farmaceuticas que los contienen en combinacion con otros agentes terapeuticos y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de aspartil-proteasas

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WO2007058602A3 (en) 2007-07-05
JP2009519221A (ja) 2009-05-14
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KR20080080565A (ko) 2008-09-04
ECSP088499A (es) 2008-07-30
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AR057984A1 (es) 2008-01-09
US20080293718A1 (en) 2008-11-27
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