JP2008508289A - 大環状βセクレターゼ阻害剤 - Google Patents

大環状βセクレターゼ阻害剤 Download PDF

Info

Publication number
JP2008508289A
JP2008508289A JP2007523724A JP2007523724A JP2008508289A JP 2008508289 A JP2008508289 A JP 2008508289A JP 2007523724 A JP2007523724 A JP 2007523724A JP 2007523724 A JP2007523724 A JP 2007523724A JP 2008508289 A JP2008508289 A JP 2008508289A
Authority
JP
Japan
Prior art keywords
compound
alkyl
effective amount
compound according
mmol
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
JP2007523724A
Other languages
English (en)
Japanese (ja)
Other versions
JP2008508289A5 (https=
Inventor
アンドリュー ダブリュー． スタムフォード，
イン ファン，
グオチン リ，
コーリー オー． ストリックランド，
ヨハネス エイチ． ボイト，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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
Application filed by Schering Corp filed Critical Schering Corp
Publication of JP2008508289A publication Critical patent/JP2008508289A/ja
Publication of JP2008508289A5 publication Critical patent/JP2008508289A5/ja
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2007523724A 2004-07-28 2005-07-26 大環状βセクレターゼ阻害剤 Pending JP2008508289A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US59189904P 2004-07-28 2004-07-28
PCT/US2005/026468 WO2006014944A1 (en) 2004-07-28 2005-07-26 Macrocyclic beta-secretase inhibitors

Publications (2)

Publication Number Publication Date
JP2008508289A true JP2008508289A (ja) 2008-03-21
JP2008508289A5 JP2008508289A5 (https=) 2008-09-04

Family

ID=35106859

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2007523724A Pending JP2008508289A (ja) 2004-07-28 2005-07-26 大環状βセクレターゼ阻害剤

Country Status (12)

Country Link
US (2) US7652003B2 (https=)
EP (1) EP1781644B1 (https=)
JP (1) JP2008508289A (https=)
CN (1) CN101027297B (https=)
AR (1) AR050184A1 (https=)
AT (1) ATE396990T1 (https=)
CA (1) CA2575340A1 (https=)
DE (1) DE602005007245D1 (https=)
ES (1) ES2306200T3 (https=)
MX (1) MX2007001102A (https=)
TW (1) TWI297337B (https=)
WO (1) WO2006014944A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008526913A (ja) * 2005-01-13 2008-07-24 ノバルティス アクチエンゲゼルシャフト Ｂａｃｅ阻害剤として有用な大環状化合物

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10303974A1 (de) 2003-01-31 2004-08-05 Abbott Gmbh & Co. Kg Amyloid-β(1-42)-Oligomere, Verfahren zu deren Herstellung und deren Verwendung
US7763609B2 (en) * 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
GB0500683D0 (en) * 2005-01-13 2005-02-23 Novartis Ag Organic compounds
MX2007016180A (es) 2005-06-14 2008-03-07 Schering Corp Inhibidores de aspartil proteasas.
JP2008543840A (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インヒビター
RU2432362C2 (ru) 2005-11-30 2011-10-27 Эбботт Лэборетриз Моноклональные антитела и их применения
PL2289909T3 (pl) 2005-11-30 2015-04-30 Abbvie Inc Sposób przeszukiwania, proces oczyszczania niedyfundujących oligomerów Abeta, selektywne przeciwciała przeciw niedyfundującym oligomerom Abeta i sposób wytwarzania tych przeciwciał
KR20090015967A (ko) 2006-06-12 2009-02-12 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제
CA2656869A1 (en) * 2006-07-20 2008-01-24 Novartis Ag Macrocyclic lactams
WO2008045250A1 (en) 2006-10-06 2008-04-17 Merck & Co., Inc. Macrocyclic spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US8455626B2 (en) 2006-11-30 2013-06-04 Abbott Laboratories Aβ conformer selective anti-aβ globulomer monoclonal antibodies
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
AU2007332754A1 (en) 2006-12-12 2008-06-19 Schering Corporation Aspartyl protease inhibitors
EP2124952A2 (en) 2007-02-27 2009-12-02 Abbott GmbH & Co. KG Method for the treatment of amyloidoses
AU2008220785B2 (en) 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
JP5667440B2 (ja) 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
WO2009032277A1 (en) 2007-09-06 2009-03-12 Schering Corporation Gamma secretase modulators
US8487099B2 (en) 2007-11-05 2013-07-16 Merck Sharp & Dohme Corp. Gamma secretase modulators
EP2227471A1 (en) 2007-12-11 2010-09-15 Schering Corporation Gamma secretase modulators
US8450331B2 (en) 2008-04-22 2013-05-28 Merck Sharp & Dohme Corp. Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
RU2011123862A (ru) 2008-11-13 2012-12-20 Шеринг Корпорейшн Модуляторы гамма-секретазы
JP2012513400A (ja) 2008-12-22 2012-06-14 シェーリング コーポレイション γ−セクレターゼ調節剤
US8759337B2 (en) 2008-12-22 2014-06-24 Merck Sharp & Dohme Corp. Gamma secretase modulators
EP2443118A1 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
WO2010147969A2 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
US20120245158A1 (en) 2009-06-16 2012-09-27 Xianhai Huang Gamma secretase modulators
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 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
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
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
JP5688745B2 (ja) 2010-03-10 2015-03-25 プロビオドルグ エージー グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤
ES2684475T3 (es) 2010-04-15 2018-10-03 Abbvie Inc. Proteínas que se unen a beta amiloide
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
CN103298833B (zh) 2010-08-14 2015-12-16 Abbvie公司 β淀粉样蛋白结合蛋白
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
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
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
AU2013235422B2 (en) 2012-03-19 2016-12-15 Buck Institute For Research On Aging APP specific BACE inhibitors (ASBIs) and uses thereof
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
EP2908825B1 (en) 2012-10-17 2018-04-18 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2014062553A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US20140371283A1 (en) 2013-02-12 2014-12-18 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
CN105175488A (zh) * 2015-09-07 2015-12-23 西北农林科技大学 一种具有抗老年痴呆症活性的化合物及其制备方法
AU2018308088B2 (en) 2017-07-25 2025-05-29 Truebinding, Inc. Treating cancer by blocking the interaction of TIM-3 and its ligand
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
AU2020214796A1 (en) 2019-01-30 2021-07-29 Truebinding, Inc. Anti-Gal3 antibodies and uses thereof
WO2021242776A2 (en) 2020-05-26 2021-12-02 Truebinding, Inc. Methods of treating inflammatory diseases by blocking galectin-3

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002100399A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
WO2002100856A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
WO2004043916A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2004062625A2 (en) * 2003-01-07 2004-07-29 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0395664A1 (en) 1987-10-21 1990-11-07 The Upjohn Company Renin inhibitors containing a (1-amino-2-hydroxy-2-heterocyclic) ethyl moiety
EP1299352B1 (en) 2000-06-30 2005-12-28 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
PE20020276A1 (es) 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
WO2002088101A2 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
US20040171614A1 (en) * 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
CA2578600A1 (en) * 2004-06-16 2006-01-26 Wyeth Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase
BRPI0512213A (pt) * 2004-06-16 2008-02-19 Wyeth Corp método para tratamento, prevenção ou melhora de uma doença ou distúrbio; composição farmacêutica; processo para a preparação de um composto; e uso de um composto
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
WO2007005404A1 (en) 2005-06-30 2007-01-11 Wyeth AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION
TW200730523A (en) 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
EP1928841A1 (en) * 2005-09-26 2008-06-11 Wyeth a Corporation of the State of Delaware Amino-5- ý4- (difluoromethoxy) phenyl¨-5-phenylimidazolone compounds as inhibitors of the beta-secretase (bace)
US20090099217A1 (en) 2006-04-05 2009-04-16 Astex Therapeutics Ltd. 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies
TW200815449A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
TW200808796A (en) 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002100399A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
WO2002100856A1 (en) * 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
WO2004043916A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2004062625A2 (en) * 2003-01-07 2004-07-29 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008526913A (ja) * 2005-01-13 2008-07-24 ノバルティス アクチエンゲゼルシャフト Ｂａｃｅ阻害剤として有用な大環状化合物

Also Published As

Publication number Publication date
US7652003B2 (en) 2010-01-26
US20100178294A1 (en) 2010-07-15
CN101027297A (zh) 2007-08-29
TWI297337B (en) 2008-06-01
US8012953B2 (en) 2011-09-06
CN101027297B (zh) 2010-09-08
EP1781644B1 (en) 2008-05-28
HK1102328A1 (en) 2007-11-16
ES2306200T3 (es) 2008-11-01
CA2575340A1 (en) 2006-02-09
DE602005007245D1 (https=) 2008-07-10
MX2007001102A (es) 2007-04-13
EP1781644A1 (en) 2007-05-09
ATE396990T1 (de) 2008-06-15
US20060040948A1 (en) 2006-02-23
TW200607807A (en) 2006-03-01
AR050184A1 (es) 2006-10-04
WO2006014944A1 (en) 2006-02-09

Similar Documents

Publication Publication Date Title
JP2008508289A (ja) 大環状βセクレターゼ阻害剤
JP2008507538A (ja) 置換アミドβセクレターゼインヒビター
JP4448134B2 (ja) ベンズアミド置換基を有する環状アミンｂａｓｅ−１阻害剤
JP4472700B2 (ja) 複素環置換基を有する環状アミンｂａｓｅ−１阻害剤
JP5020638B2 (ja) 複素環式アスパルチルプロテアーゼインヒビター
JP7264810B2 (ja) アルファｖインテグリン阻害剤としてのシクロブタン－およびアゼチジン－含有の単環およびスピロ環式化合物
TW200948364A (en) Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
JP2007513973A5 (https=)
CN104870000A (zh) 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途
US20230303552A1 (en) Arylsulfonyl derivatives and their use as muscarinic acetylcholine receptor m5 inhibitors
US20240182445A1 (en) Modulators of trek (twik related k+ channels) channel function
HK1102328B (en) Macrocyclic beta-secretase inhibitors
WO2023150526A1 (en) Competitive and noncompetitive octahydrocyclopenta[c]pyrrole inhibitors of the muscarinic acetylcholine receptor m5
WO2023150525A1 (en) Competitive and noncompetitive piperidine sulfonyl inhibitors of the muscarinic acetylcholine receptor m5

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20080718

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20080718

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110921

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20120307