IL111078A - Inhibitors of protein production in amyloid, a process for their preparation and pharmaceutical preparations containing them - Google Patents

Inhibitors of protein production in amyloid, a process for their preparation and pharmaceutical preparations containing them

Info

Publication number
IL111078A
IL111078A IL11107894A IL11107894A IL111078A IL 111078 A IL111078 A IL 111078A IL 11107894 A IL11107894 A IL 11107894A IL 11107894 A IL11107894 A IL 11107894A IL 111078 A IL111078 A IL 111078A
Authority
IL
Israel
Prior art keywords
benzyl
aryl
alkyl
group
mmol
Prior art date
Application number
IL11107894A
Other languages
English (en)
Hebrew (he)
Other versions
IL111078A0 (en
Original Assignee
Merrell Dow Pharma
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 Merrell Dow Pharma filed Critical Merrell Dow Pharma
Publication of IL111078A0 publication Critical patent/IL111078A0/xx
Publication of IL111078A publication Critical patent/IL111078A/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Psychiatry (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)
IL11107894A 1993-10-01 1994-09-29 Inhibitors of protein production in amyloid, a process for their preparation and pharmaceutical preparations containing them IL111078A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP93402398 1993-10-01

Publications (2)

Publication Number Publication Date
IL111078A0 IL111078A0 (en) 1994-11-28
IL111078A true IL111078A (en) 1999-03-12

Family

ID=8214751

Family Applications (1)

Application Number Title Priority Date Filing Date
IL11107894A IL111078A (en) 1993-10-01 1994-09-29 Inhibitors of protein production in amyloid, a process for their preparation and pharmaceutical preparations containing them

Country Status (19)

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

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US6008196A (en) * 1994-06-02 1999-12-28 Hoechst Marion Roussel, Inc. Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
JP4221059B2 (ja) * 1994-06-02 2009-02-12 アベンティス・インコーポレイテッド エラスターゼインヒビターのプロドラッグとしてのアシル化エノール誘導体
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
US5783434A (en) * 1995-06-06 1998-07-21 Tung; Jay S. Cathepsin and methods and compositions for inhibition thereof
US5849711A (en) * 1995-06-06 1998-12-15 Athena Neurosciences, Inc. 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 (fr) 1995-12-05 1997-06-06 Kevin Felsenstein Derives de 5-amino-6-cyclohexyl-4-hydroxyhexanamide, inhibiteurs de la production de proteine .beta.-amyloide
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
US6207710B1 (en) 1996-11-22 2001-03-27 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
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
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
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6211235B1 (en) 1996-11-22 2001-04-03 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
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
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
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
HUP0001383A3 (en) * 1996-11-22 2001-11-28 Lilly Co Eli N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions comprising same and their use
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
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
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
US6958330B1 (en) 1998-06-22 2005-10-25 Elan Pharmaceuticals, Inc. Polycyclic α-amino-ε-caprolactams and related 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
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
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
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
US6395897B1 (en) 1999-03-02 2002-05-28 Boehringer Ingelheim Pharmaceuticals, Inc. Nitrile compounds useful as reversible inhibitors of #9 cathepsin 5
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
WO2001087354A2 (fr) 2000-05-17 2001-11-22 Bristol-Myers Squibb Pharma Company Utilisation de radioligands a petites molecules en vue de rechercher des inhibiteurs de production d'amyloide-beta et destine a l'imagerie diagnostique
US6613801B2 (en) 2000-05-30 2003-09-02 Transtech Pharma, Inc. Method for the synthesis of compounds of formula I and their uses thereof
BR0106717A (pt) 2000-06-01 2002-04-16 Bristol Myers Squibb Pharma Co Compostos, composição farmacêutica e usos dos compostos de lactama inovadora
US6432944B1 (en) 2000-07-06 2002-08-13 Bristol-Myers Squibb Company Benzodiazepinone β-amyloid inhibitors: arylacetamidoalanyl derivatives
CA2440042C (fr) 2001-03-05 2011-09-27 Transtech Pharma, Inc. Derives de carboxamide utilises comme agents therapeutiques
JP2004523565A (ja) 2001-03-05 2004-08-05 トランス　テック　ファーマ，インコーポレイテッド 治療因子としてのベンゾイミダゾール誘導体
CN101613321A (zh) 2002-03-05 2009-12-30 特兰斯泰克制药公司 抑制配体与高级糖化终产物受体相互作用的单和双环吡咯衍生物
US7223745B2 (en) 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
KR100851035B1 (ko) 2005-08-23 2008-08-11 대한민국 ＧＣＰ-Ⅱ를 유효성분으로 함유하는 β-아밀로이드의 뇌내축적 예방 및 치료용 약학적 조성물과 치료제 스크리닝용조성물 및 이를 이용한 스크리닝 방법
CA2772797C (fr) 2009-09-30 2018-09-25 Transtech Pharma, Inc. Derives d'imidazole substitues
AU2010341530B2 (en) 2009-12-22 2016-03-10 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
US9717710B2 (en) 2012-10-05 2017-08-01 Vtv Therapeutics Llc Treatment of mild and moderate Alzheimer's disease
EP3385266B1 (fr) 2015-12-30 2019-08-14 Neuboron Medtech Ltd. Composé pour liaison spécifique avec protéine bêta-amyloïde
CN114685453A (zh) 2016-06-21 2022-07-01 奥瑞恩眼科有限责任公司 杂环脯氨酰胺衍生物
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
CN111867549B (zh) * 2018-02-02 2024-01-05 安捷伦科技有限公司 用于使用封闭的2-aa进行聚糖分析的方法和试剂盒
WO2019190822A1 (fr) 2018-03-28 2019-10-03 Vtv Therapeutics Llc Formes cristallines de [3-(4- {2-butyl-1-[4-(4-chloro-phénoxy)-phényl]-1h-imidazol-4-yl} -phénoxy)-propyl]-diéthyl-amine
WO2019190823A1 (fr) 2018-03-28 2019-10-03 Vtv Therapeutics Llc Sels pharmaceutiquement acceptables de [3-(4- {2-butyl-1-[4-(4-chlorophénoxy)-phényl]-1h-imidazol-4-yl} -phénoxy)-propyl]-diéthyl-amine
WO2020076668A1 (fr) 2018-10-10 2020-04-16 Vtv Therapeutics Llc Métabolites de [3-(4-{2-butyl-1-[4-(4-chloro-phénoxy)-phényl]-1h-imidazol-4-yl}-phénoxy)-propyl]-diéthyl-amine

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5142056A (en) * 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
ZA86746B (en) * 1985-02-04 1986-09-24 Merrell Dow Pharma Novel peptidase inhibitors
CA2021660A1 (fr) * 1989-07-26 1991-01-27 Philippe Bey Inhibiteurs de la peptidose
WO1992014696A2 (fr) * 1991-02-22 1992-09-03 The Du Pont Merck Pharmaceutical Company α-AMINOALDEHYDES SUBSTITUES ET LEURS DERIVES
CA2071621C (fr) * 1991-06-19 1996-08-06 Ahihiko Hosoda Derives d'aldehyde

Also Published As

Publication number Publication date
ATE211129T1 (de) 2002-01-15
CA2171882A1 (fr) 1995-04-13
ES2170104T3 (es) 2002-08-01
AU7799894A (en) 1995-05-01
DE69429527D1 (de) 2002-01-31
JPH09505281A (ja) 1997-05-27
KR960704839A (ko) 1996-10-09
AU687449B2 (en) 1998-02-26
ZA947529B (en) 1995-05-29
EP0721449A1 (fr) 1996-07-17
IL111078A0 (en) 1994-11-28
CA2171882C (fr) 2001-12-04
FI961438A (fi) 1996-03-29
DE69429527T2 (de) 2002-07-18
KR100316865B1 (ko) 2002-11-29
EP0721449B1 (fr) 2001-12-19
CN1132504A (zh) 1996-10-02
HUT74004A (en) 1996-10-28
DK0721449T3 (da) 2002-04-22
NO961326D0 (no) 1996-04-01
FI961438A0 (fi) 1996-03-29
TW264480B (fr) 1995-12-01
HU9600832D0 (en) 1996-05-28
PT721449E (pt) 2002-06-28
WO1995009838A1 (fr) 1995-04-13
CN1078886C (zh) 2002-02-06
HU221629B1 (hu) 2002-12-28
NO308029B1 (no) 2000-07-10
NO961326L (no) 1996-04-01
NZ274074A (en) 1997-11-24

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Owner name: AVENTIS INC.

Free format text: FORMER NAME:MERRELL PHARMACEUTICALS INC.

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