KR100316865B1 - 베타-아밀로이드단백질생성억제제 - Google Patents

베타-아밀로이드단백질생성억제제 Download PDF

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Publication number
KR100316865B1
KR100316865B1 KR1019960701686A KR19960701686A KR100316865B1 KR 100316865 B1 KR100316865 B1 KR 100316865B1 KR 1019960701686 A KR1019960701686 A KR 1019960701686A KR 19960701686 A KR19960701686 A KR 19960701686A KR 100316865 B1 KR100316865 B1 KR 100316865B1
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South Korea
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alkyl
benzyl
aryl
nhc
group
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Expired - Fee Related
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KR1019960701686A
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English (en)
Korean (ko)
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KR960704839A (ko
Inventor
코델 바바라
쉬르렝 다니엘
피. 피트 노톤
엔. 히가키 제프리
방 도르셀라에 비비안느
알. 앤젤라스트로 마이클
Original Assignee
메렐 파마슈티칼스 인크.
시오스 노바 인코포레이티드
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Publication of KR960704839A publication Critical patent/KR960704839A/ko
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Publication of KR100316865B1 publication Critical patent/KR100316865B1/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
KR1019960701686A 1993-10-01 1994-09-20 베타-아밀로이드단백질생성억제제 Expired - Fee Related KR100316865B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP93402398 1993-10-01
EP93402398.7 1993-10-01
PCT/US1994/010679 WO1995009838A1 (en) 1993-10-01 1994-09-20 INHIBITORS OF β-AMYLOID PROTEIN PRODUCTION

Publications (2)

Publication Number Publication Date
KR960704839A KR960704839A (ko) 1996-10-09
KR100316865B1 true KR100316865B1 (ko) 2002-11-29

Family

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KR1019960701686A Expired - Fee Related KR100316865B1 (ko) 1993-10-01 1994-09-20 베타-아밀로이드단백질생성억제제

Country Status (19)

Country Link
EP (1) EP0721449B1 (enExample)
JP (1) JPH09505281A (enExample)
KR (1) KR100316865B1 (enExample)
CN (1) CN1078886C (enExample)
AT (1) ATE211129T1 (enExample)
AU (1) AU687449B2 (enExample)
CA (1) CA2171882C (enExample)
DE (1) DE69429527T2 (enExample)
DK (1) DK0721449T3 (enExample)
ES (1) ES2170104T3 (enExample)
FI (1) FI961438A0 (enExample)
HU (1) HU221629B1 (enExample)
IL (1) IL111078A (enExample)
NO (1) NO308029B1 (enExample)
NZ (1) NZ274074A (enExample)
PT (1) PT721449E (enExample)
TW (1) TW264480B (enExample)
WO (1) WO1995009838A1 (enExample)
ZA (1) ZA947529B (enExample)

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PT762887E (pt) * 1994-06-02 2002-01-30 Merrell Pharma Inc Derivados do enol acetilado como pro-farmacos de inibidores de elastase
EP0763055B1 (en) * 1994-06-02 1999-11-03 Merrell Pharmaceuticals Inc. Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
US5804560A (en) * 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US5691368A (en) * 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
US5849711A (en) * 1995-06-06 1998-12-15 Athena Neurosciences, Inc. Cathepsin and methods and compositions for inhibition thereof
US5783434A (en) * 1995-06-06 1998-07-21 Tung; Jay S. Cathepsin and methods and compositions for inhibition thereof
JPH11506923A (ja) * 1995-06-06 1999-06-22 アセナ ニューロサイエンシーズ，インコーポレイテッド 新しいカテプシンならびにその阻害のための方法および組成物
US6172044B1 (en) 1995-12-01 2001-01-09 Aventis Pharmaceuticals Inc. Acylated enol derivative of α-ketoesters and α-ketoamides
CA2191924A1 (en) 1995-12-05 1997-06-06 Kevin Felsenstein 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of .beta.-amyloid protein production
US5703129A (en) * 1996-09-30 1997-12-30 Bristol-Myers Squibb Company 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production
US6117901A (en) 1996-11-22 2000-09-12 Athena Neurosciences, Inc. N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for use
US6211235B1 (en) 1996-11-22 2001-04-03 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
AR016751A1 (es) * 1996-11-22 2001-08-01 Athena Neurosciences Inc Metodo para inhibir la liberacion del peptido beta-amiloide en una celula, composicion farmaceutica y compuestos utiles en dicho metodo
US6207710B1 (en) 1996-11-22 2001-03-27 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6096782A (en) * 1996-11-22 2000-08-01 Athena Neurosciences, Inc. N-(aryl/heteroaryl) amino acid derivatives pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6642261B2 (en) 1997-11-21 2003-11-04 Athena Neurosciences, Inc. N-(aryl/heteroarylacety) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6153652A (en) 1996-11-22 2000-11-28 Elan Pharmaceuticals, Inc. N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
TR199901132T2 (xx) * 1996-11-22 1999-08-23 Elan Pharmaceuticals, Inc. N-(aril/heteoaril) amino asit t�revleri, bunlar� i�eren farmas�tik bile�imler ve b�yle bile�ikler kullan�larak �-amiloid peptidinin sal�nmas�n� ve/veya sentezini inhibe etmek i�in y�ntemler.
DE19648793A1 (de) 1996-11-26 1998-05-28 Basf Ag Neue Benzamide und deren Anwendung
US6635632B1 (en) 1996-12-23 2003-10-21 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6683075B1 (en) 1996-12-23 2004-01-27 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use
US6506782B1 (en) 1998-02-27 2003-01-14 Athena Neurosciences, Inc. Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6569851B1 (en) 1998-06-22 2003-05-27 Elan Pharmaceutials, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6552013B1 (en) 1998-06-22 2003-04-22 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6958330B1 (en) 1998-06-22 2005-10-25 Elan Pharmaceuticals, Inc. Polycyclic α-amino-ε-caprolactams and related compounds
US6774125B2 (en) 1998-06-22 2004-08-10 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6509331B1 (en) 1998-06-22 2003-01-21 Elan Pharmaceuticals, Inc. Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6528505B1 (en) 1998-06-22 2003-03-04 Elan Pharmaceuticals, Inc. Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6737038B1 (en) 1998-11-12 2004-05-18 Bristol-Myers Squibb Company Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
CA2360740A1 (en) 1999-03-02 2000-09-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cathepsin s
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US6878363B2 (en) 2000-05-17 2005-04-12 Bristol-Myers Squibb Pharma Company Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
US6613801B2 (en) * 2000-05-30 2003-09-02 Transtech Pharma, Inc. Method for the synthesis of compounds of formula I and their uses thereof
US7361678B2 (en) 2002-03-05 2008-04-22 Transtech Pharma, Inc. Azole derivatives and fused bicyclic azole derivatives as therapeutic agents
WO2001092235A1 (en) 2000-06-01 2001-12-06 Bristol-Myers Squibb Pharma Company LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
US6432944B1 (en) 2000-07-06 2002-08-13 Bristol-Myers Squibb Company Benzodiazepinone β-amyloid inhibitors: arylacetamidoalanyl derivatives
AU2002245590B2 (en) 2001-03-05 2006-06-29 Transtech Pharma, Inc. Benzimidazole derivatives as therapeutic agents
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US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
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US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
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CA2772797C (en) 2009-09-30 2018-09-25 Transtech Pharma, Inc. Substituted imidazole derivatives
CN102725300B (zh) 2009-12-22 2015-03-11 赛福伦公司 蛋白酶体抑制剂及其制备、纯化、和应用的方法
US9717710B2 (en) 2012-10-05 2017-08-01 Vtv Therapeutics Llc Treatment of mild and moderate Alzheimer's disease
CN108530473A (zh) * 2015-12-30 2018-09-14 南京中硼联康医疗科技有限公司 和β淀粉样蛋白特异性结合的化合物
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
MX392422B (es) 2016-06-21 2025-03-24 Orion Ophthalmology LLC Derivados de prolinamida heterociclica
WO2019152724A1 (en) * 2018-02-02 2019-08-08 Prozyme, Inc. Methods and kits for using blocked 2-aa for glycan analysis
WO2019190822A1 (en) 2018-03-28 2019-10-03 Vtv Therapeutics Llc Crystalline forms of [3-(4- {2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1h-imidazol-4-yl} -phenoxy)-propyl]-diethyl-amine
WO2019190823A1 (en) 2018-03-28 2019-10-03 Vtv Therapeutics Llc Pharmaceutically acceptable salts of [3-(4- {2-butyl-1-[4-(4-chlorophenoxy)-phenyl]-1h-imidazol-4-yl} -phenoxy)-propyl]-diethyl-amine
WO2020076668A1 (en) 2018-10-10 2020-04-16 Vtv Therapeutics Llc Metabolites of [3-(4-{2-butyl-l-[4-(4-chloro-phenoxy)-phenyl]-lh-imidazol-4-yl } -phen ox y)-prop yl] -diethyl-amine

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CA1341029C (en) * 1985-02-04 2000-06-20 Michael Kolb Peptidase inhibitors
ZA905737B (en) * 1989-07-26 1991-05-29 Merrell Dow Pharma Novel peptidase inhibitors
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CA2071621C (en) * 1991-06-19 1996-08-06 Ahihiko Hosoda Aldehyde derivatives

Also Published As

Publication number Publication date
NO308029B1 (no) 2000-07-10
TW264480B (enExample) 1995-12-01
CA2171882A1 (en) 1995-04-13
DE69429527T2 (de) 2002-07-18
KR960704839A (ko) 1996-10-09
AU7799894A (en) 1995-05-01
AU687449B2 (en) 1998-02-26
EP0721449B1 (en) 2001-12-19
HU9600832D0 (en) 1996-05-28
CN1132504A (zh) 1996-10-02
NO961326L (no) 1996-04-01
ZA947529B (en) 1995-05-29
FI961438L (fi) 1996-03-29
DK0721449T3 (da) 2002-04-22
CN1078886C (zh) 2002-02-06
PT721449E (pt) 2002-06-28
HUT74004A (en) 1996-10-28
NZ274074A (en) 1997-11-24
DE69429527D1 (de) 2002-01-31
HU221629B1 (hu) 2002-12-28
ES2170104T3 (es) 2002-08-01
IL111078A0 (en) 1994-11-28
EP0721449A1 (en) 1996-07-17
JPH09505281A (ja) 1997-05-27
ATE211129T1 (de) 2002-01-15
FI961438A7 (fi) 1996-03-29
NO961326D0 (no) 1996-04-01
WO1995009838A1 (en) 1995-04-13
CA2171882C (en) 2001-12-04
FI961438A0 (fi) 1996-03-29
IL111078A (en) 1999-03-12

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