PE52799A1 - Cicloalquilo, lactama, lactona y compuestos relacionados, composiciones farmaceuticas que comprenden los mismos, como inhibidores de la liberacion de peptido �-amiloide y no cicloalquilo, lactama, lactona y compuestos relacionados, como inhibidores de la liberacion del peptido �-amiloide - Google Patents

Cicloalquilo, lactama, lactona y compuestos relacionados, composiciones farmaceuticas que comprenden los mismos, como inhibidores de la liberacion de peptido �-amiloide y no cicloalquilo, lactama, lactona y compuestos relacionados, como inhibidores de la liberacion del peptido �-amiloide

Info

Publication number
PE52799A1
PE52799A1 PE1997001158A PE00115897A PE52799A1 PE 52799 A1 PE52799 A1 PE 52799A1 PE 1997001158 A PE1997001158 A PE 1997001158A PE 00115897 A PE00115897 A PE 00115897A PE 52799 A1 PE52799 A1 PE 52799A1
Authority
PE
Peru
Prior art keywords
lactam
lactone
related compounds
cycloalkyl
laiber
Prior art date
Application number
PE1997001158A
Other languages
English (en)
Inventor
James E Audia
Thomas C Britton
James J Droste
Lee H Latimer
Thomas E Mabry
Jeffrey S Nissen
Warren J Porter
Jon K Reel
Eugene D Thorsett
Jay S Tung
Jing Wu
William Leonard Scott
Michael A Pleiss
Jeffrey Neitz
Stephen Freedman
Bruce A Dressman
Cynthia L Cwi
Steven S Henry
Stacey L Mcdaniel
Russell D Stucky
Varghese John
Original Assignee
Athena Neurosciences Inc
Lilly Co Eli
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 Athena Neurosciences Inc, Lilly Co Eli filed Critical Athena Neurosciences Inc
Publication of PE52799A1 publication Critical patent/PE52799A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/78—Ring systems having three or more relevant rings
    • C07D311/80—Dibenzopyrans; Hydrogenated dibenzopyrans
    • C07D311/82—Xanthenes
    • C07D311/90—Xanthenes with hydrocarbon radicals, substituted by amino radicals, directly attached in position 9
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/08—Oxygen atoms
    • C07D223/10—Oxygen atoms attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/12—1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D281/02—Seven-membered rings
    • C07D281/04—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D281/08—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D281/10—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D307/32—Oxygen atoms
    • C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/005—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1021—Tetrapeptides with the first amino acid being acidic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/14—All rings being cycloaliphatic
    • C07C2602/32—All rings being cycloaliphatic the ring system containing at least eleven carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/30—Ortho- or ortho- and peri-condensed systems containing three rings containing seven-membered rings
    • C07C2603/32—Dibenzocycloheptenes; Hydrogenated dibenzocycloheptenes
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2770/00—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA ssRNA viruses positive-sense
    • C12N2770/00011—Details
    • C12N2770/24011—Flaviviridae
    • C12N2770/24211—Hepacivirus, e.g. hepatitis C virus, hepatitis G virus
    • C12N2770/24222—New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Genetics & Genomics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

SE REFIEREN A COMPUESTOS (I), EN DONDE: R1 ES FENILO o HETEROARILO, ENTRE OTROS; "W" Y C(H)pC(=X) FORMAN UN CICLOALQUILO, HETEROCICLO, ENTRE OTROS; "X" ES =O, =S, (H,OH), (H,SH) e (H,H); "Y" ES CH(R2)-CO-NH; R2 ES ALQUILO, CICLOALQUILO, ENTRE OTROS; "Z" ES TCX`X"CO; "T" ES UN ENLACE; X' Y X" SON H, OH, F o AMBOS FORMAN =O; m Y p SON 0-1; n ES 0-2; CON LA CONDICION DE QUE a)CUANDO R1 ES 3,5-DIFLUOROFENILO, R2 ES CH3, "Z" ES CH2CO, m, n Y p SON 1 ENTONCES W Y CH Y C=X NO FORMAN UN GRUPO 2-(S)-INDANOL, ENTRE OTRAS CONDICIONES LOS COMPUESTOS (I) PUEDEN SER UTILES EN EL TRATAMIENTO Y PREVENCION DE LA ENFERMEDAD DE ALZHEIMER
PE1997001158A 1996-12-23 1997-12-23 Cicloalquilo, lactama, lactona y compuestos relacionados, composiciones farmaceuticas que comprenden los mismos, como inhibidores de la liberacion de peptido �-amiloide y no cicloalquilo, lactama, lactona y compuestos relacionados, como inhibidores de la liberacion del peptido �-amiloide PE52799A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US78002596A 1996-12-23 1996-12-23

Publications (1)

Publication Number Publication Date
PE52799A1 true PE52799A1 (es) 1999-05-27

Family

ID=25118329

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997001158A PE52799A1 (es) 1996-12-23 1997-12-23 Cicloalquilo, lactama, lactona y compuestos relacionados, composiciones farmaceuticas que comprenden los mismos, como inhibidores de la liberacion de peptido �-amiloide y no cicloalquilo, lactama, lactona y compuestos relacionados, como inhibidores de la liberacion del peptido �-amiloide

Country Status (28)

Country Link
EP (1) EP0951466B1 (es)
JP (1) JP3812952B2 (es)
KR (1) KR20000069654A (es)
CN (2) CN1616432A (es)
AR (1) AR010854A1 (es)
AT (1) ATE421509T1 (es)
AU (1) AU749658C (es)
BR (1) BR9714517A (es)
CA (1) CA2272305A1 (es)
CO (1) CO4930282A1 (es)
DE (1) DE69739236D1 (es)
DK (1) DK0951466T3 (es)
EA (1) EA002100B1 (es)
ES (1) ES2319239T3 (es)
HR (1) HRP970705A2 (es)
HU (1) HUP0001232A3 (es)
ID (1) ID22177A (es)
IL (2) IL158355A0 (es)
NO (1) NO993098L (es)
NZ (1) NZ335583A (es)
PE (1) PE52799A1 (es)
PL (1) PL196641B1 (es)
PT (1) PT951466E (es)
SI (1) SI0951466T1 (es)
TR (1) TR199901343T2 (es)
TW (1) TW568914B (es)
WO (1) WO1998028268A2 (es)
ZA (1) ZA9711537B (es)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003521438A (ja) * 1997-12-22 2003-07-15 エラン ファーマシューティカルズ，インコーポレイテッド 多環式α−アミノ−ε−カプロラクタムおよび関連化合物
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
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
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
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
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
NZ525513A (en) 1998-08-07 2004-09-24 Pont Pharmaceuticals Du Succinoylamino lactams as inhibitors of Abeta protein production
EP1131634A2 (en) * 1998-09-30 2001-09-12 Elan Pharmaceuticals, Inc. Determining the mechanism of beta-amyloid peptide generation
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
CN1636011A (zh) * 1998-12-24 2005-07-06 杜邦药品公司 作为Aβ蛋白产生抑制剂的琥珀酰氨基苯并二氮杂䓬
WO2001002358A2 (en) * 1999-07-06 2001-01-11 Vertex Pharmaceuticals Incorporated Cyclized amide derivatives for treating or preventing neuronal damage
JP2003506440A (ja) * 1999-08-05 2003-02-18 プレサイエント ニューロファーマ インコーポレイテッド 中枢神経系に関連する疾患の処置のための１，４−ジアゼピン誘導体
US6960576B2 (en) 1999-09-13 2005-11-01 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
CN1399634A (zh) 1999-09-13 2003-02-26 布里斯托尔-迈尔斯斯奎布药品公司 用作Aβ蛋白生成抑制剂的羟基链烷醇氨基内酰胺和相关结构
US6503902B2 (en) 1999-09-13 2003-01-07 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of a β protein production
AU7997700A (en) 1999-10-08 2001-04-23 Du Pont Pharmaceuticals Company Amino lactam sulfonamides as inhibitors of abeta protein production
CA2390376A1 (en) * 1999-11-09 2001-05-17 William Leonard Scott .beta.-aminoacid compounds useful for inhibiting .beta.-amyloid peptide release and/or its synthesis
CA2395862A1 (en) * 2000-02-17 2001-08-23 Hong Liu Succinoylamino carbocycles and heterocycles as inhibitors of a.beta. protein production
AU2001249477A1 (en) * 2000-03-28 2001-10-08 Bristol-Myers Squibb Pharma Company Lactams as inhibitors of a-beta protein production
US6495540B2 (en) 2000-03-28 2002-12-17 Bristol - Myers Squibb Pharma Company Lactams as inhibitors of A-β protein production
IL151576A0 (en) * 2000-04-03 2003-04-10 Bristol Myers Squibb Pharma Co Cyclic lactams as inhibitors of a-beta protein production
CN1434803A (zh) * 2000-04-03 2003-08-06 布里斯托尔-迈尔斯斯奎布药品公司 作为Aβ蛋白质产生抑制剂的环内酰胺
AU2001257006A1 (en) 2000-04-11 2001-10-23 Du Pont Pharmaceuticals Company Substituted lactams as inhibitors of abeta protein production
AU2001261728A1 (en) 2000-05-17 2001-11-26 Bristol-Myers Squibb Pharma Company Use of small molecule radioligands for diagnostic imaging
GB0012671D0 (en) 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents
CA2379445C (en) 2000-06-01 2007-08-21 Bristol-Myers Squibb Pharma Company Lactams substituted by cyclic succinates as inhibitors of a.beta. protein production
US6432944B1 (en) 2000-07-06 2002-08-13 Bristol-Myers Squibb Company Benzodiazepinone β-amyloid inhibitors: arylacetamidoalanyl derivatives
GB0025173D0 (en) 2000-10-13 2000-11-29 Merck Sharp & Dohme Therapeutic agents
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
UA77165C2 (en) * 2000-11-17 2006-11-15 Lilly Co Eli (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition
US7468365B2 (en) 2000-11-17 2008-12-23 Eli Lilly And Company Lactam compound
CA2425558C (en) * 2000-11-17 2012-01-03 Eli Lilly And Company Lactam compound
WO2002057249A1 (en) * 2001-01-17 2002-07-25 Amura Therapeutics Limited Cyclic 2-carbonylaminoketones as inhibitors of cruzipain and other cysteine proteases
US7132449B2 (en) 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
ATE356130T1 (de) 2001-01-17 2007-03-15 Amura Therapeutics Ltd Inhibitoren von cruzipain und anderen cysteinproteasen
IL156776A0 (en) 2001-01-17 2004-02-08 Amura Therapeutics Ltd Inhibitors of cruzipain and other cysteine proteases
AR039059A1 (es) 2001-08-06 2005-02-09 Sanofi Aventis Compuesto derivado de acilaminotiazol, su utilizacion, procedimientos para prepararlo, composicion farmaceutica que lo comprende, y compuestos intermediarios
FR2840899B1 (fr) * 2002-06-12 2005-02-25 Sanofi Synthelabo Derives d'acylaminothiazole, leur preparation et leur utilisation en therapeutique
TW200502221A (en) * 2002-10-03 2005-01-16 Astrazeneca Ab Novel lactams and uses thereof
JP2006514110A (ja) * 2002-11-11 2006-04-27 バイエル・ヘルスケア・アクチェンゲゼルシャフト Ｉｐ受容体アンタゴニストとしてのフェニルまたはヘテロアリールアミノアルカン誘導体
WO2004058717A1 (en) 2002-12-20 2004-07-15 X-Ceptor Therapeutics, Inc. Isoquinolinone derivatives and their use as therapeutic agents
FR2850380B1 (fr) 2003-01-23 2006-07-07 Sanofi Synthelabo Derives d'acylaminothiazole, leur preparation et leur utilisation en therapeutique
US7342007B2 (en) 2003-03-14 2008-03-11 Astrazeneca Ab Lactams and uses thereof
US7432379B2 (en) 2003-05-02 2008-10-07 Elan Pharmaceuticals, Inc. Substituted pyrazole derivatives and related compounds as bradykinin B1 receptor antagonists
ITMI20032278A1 (it) 2003-11-21 2005-05-22 Ethicon Endo Surgery Inc Dispositivo di diagnosi
JP5248779B2 (ja) * 2003-12-01 2013-07-31 ケンブリッジ エンタープライズ リミティド 抗炎症剤
ES2375627T3 (es) 2004-02-23 2012-03-02 Eli Lilly And Company Anticuerpos anti-abeta.
EP2433634A3 (en) 2004-09-17 2012-07-18 The Whitehead Institute for Biomedical Research Compounds, compositions and methods of inhibiting a-synuclein toxicity
JP4519621B2 (ja) * 2004-11-30 2010-08-04 アイバイツ株式会社 光酸発生剤および感光性樹脂組成物
WO2008076556A2 (en) 2006-11-15 2008-06-26 Massachusetts Eye & Ear Infirmary Generation of inner ear cells
AU2008215948A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of AD and related conditions
CN101284828B (zh) * 2007-04-12 2011-04-27 中国科学院上海药物研究所 环庚烷并吡啶类化合物、其制备方法、用途及包含此类化合物的药物组合物
BRPI0815135A2 (pt) 2007-08-14 2015-02-03 Lilly Co Eli Derivados de azepina como inibidores de gama secretase.
US8354446B2 (en) 2007-12-21 2013-01-15 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (SARMs) and uses thereof
US8461389B2 (en) 2008-04-18 2013-06-11 University College Dublin, National University Of Ireland, Dublin Psycho-pharmaceuticals
US9776963B2 (en) 2008-11-10 2017-10-03 The Trustees Of The University Of Pennsylvania Small molecule CD4 mimetics and uses thereof
CA2743436C (en) 2008-11-24 2017-10-31 Massachusetts Eye & Ear Infirmary Pathways to generate hair cells
US20110319396A1 (en) * 2009-01-23 2011-12-29 Msd K.K. Benzodiazepin-2-on derivatives
JP2012517997A (ja) * 2009-02-17 2012-08-09 Ｍｓｄ株式会社 １，４−ベンゾジアゼピン−２−オン誘導体
AR079170A1 (es) 2009-12-10 2011-12-28 Lilly Co Eli Compuesto de ciclopropil-benzamida-imidazo-benzazepina inhibidor de diacil-glicerol aciltransferasa, sal del mismo, composicion farmaceutica que lo comprende, su uso para preparar un medicamento util para el tratamiento de obesidad o para mejorar la sensibilidad a insulina y compuesto intermedio par
US8486967B2 (en) * 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9422292B2 (en) 2011-05-04 2016-08-23 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
JO3148B1 (ar) * 2011-07-27 2017-09-20 Lilly Co Eli مركب مثبط لإشارات مسار notch
WO2013090696A1 (en) 2011-12-14 2013-06-20 Dana-Farber Cancer Institute, Inc. Cd4-mimetic inhibitors of hiv-1 entry and methods of use thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
EP3970725A1 (en) 2012-09-07 2022-03-23 Massachusetts Eye & Ear Infirmary A gamma secretase inhibitor for treating hearing loss
CN103435549A (zh) * 2013-08-14 2013-12-11 无锡惠飞生物医药技术有限公司 5-甲基-7-氨基-5H,7H-二苯并[b,d]氮杂环庚-6-酮的制备方法
EP3613418A1 (en) 2014-01-17 2020-02-26 Ligand Pharmaceuticals, Inc. Methods and compositions for modulating hormone levels
CA2952830C (en) 2014-06-20 2022-11-01 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
WO2016022776A2 (en) 2014-08-06 2016-02-11 Massachusetts Eye And Ear Infirmary Increasing atoh1 life to drive sensorineural hair cell differentiantion
US9975848B2 (en) 2014-08-13 2018-05-22 The Trustees Of The University Of Pennsylvania Inhibitors of HIV-1 entry and methods of use thereof
EP3212773B1 (en) 2014-10-29 2021-09-15 Massachusetts Eye and Ear Infirmary Efficient delivery of therapeutic molecules to cells of the inner ear
TWI609687B (zh) 2015-04-14 2018-01-01 美國禮來大藥廠 平滑肌肉瘤之標靶性治療
WO2017096233A1 (en) 2015-12-04 2017-06-08 Massachusetts Eye And Ear Infirmary Treatment of hearing loss by inhibition of casein kinase 1
AU2017212655B2 (en) 2016-01-29 2024-01-18 Decibel Therapeutics, Inc. Expansion and differentiation of inner ear supporting cells and methods of use thereof
MX2018012457A (es) 2016-04-12 2019-03-07 Lilly Co Eli Terapia combinatoria con inhibidores notch y cdk4/6.
JP6911048B2 (ja) 2016-04-12 2021-07-28 イーライ リリー アンド カンパニー がんの処置において使用するための、Ｎｏｔｃｈ阻害剤およびＰＩ３Ｋ／ｍＴＯＲ阻害剤を用いた併用療法
CA3024424A1 (en) 2016-05-16 2017-11-23 The General Hospital Corporation Human airway stem cells in lung epithelial engineering
BR112018073673A2 (pt) 2016-05-20 2019-02-26 Eli Lilly And Company terapia de combinação com inibidores de notch e de pd-1 ou pd-l1
CN106243050B (zh) * 2016-08-10 2019-09-06 安徽恒星制药有限公司 一种适合工业化生产氯巴占的方法
EP3525796A1 (en) 2016-10-12 2019-08-21 Eli Lilly and Company Targeted treatment of mature t-cell lymphoma
RU2757276C2 (ru) 2016-12-16 2021-10-12 Пайплайн Терапьютикс, Инк. Способы лечения кохлеарной синаптопатии
IL268349B1 (en) 2017-02-17 2024-04-01 Hutchinson Fred Cancer Res Combination therapies for the treatment of BCMA-associated cancer and autoimmune disorders
WO2019148067A1 (en) 2018-01-26 2019-08-01 Massachusetts Eye And Ear Infirmary Treatment of hearing loss
CN113754616B (zh) * 2021-09-27 2023-07-18 北京工商大学 一种反式-3-苯硫基-γ-内酯的制备方法
CN116116396B (zh) * 2023-02-20 2023-11-14 哈尔滨工程大学 一种偕胺肟基凝胶/氧化石墨/海绵复合材料的制备方法和应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU505133B2 (en) * 1973-12-28 1979-11-08 Fujisawa Pharmaceutical Co., Ltd Azetidinone derivatives
FR2278335A1 (fr) * 1974-07-04 1976-02-13 Fujisawa Pharmaceutical Co Derives d'azetidinones et leurs procedes de preparation
CZ184194A3 (en) * 1993-08-09 1995-03-15 Lilly Co Eli Aspartylprotease inhibitor and method of identifying thereof
US5580979A (en) * 1994-03-15 1996-12-03 Trustees Of Tufts University Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions
US6251928B1 (en) * 1994-03-16 2001-06-26 Eli Lilly And Company Treatment of alzheimer's disease employing inhibitors of cathepsin D
US5849691A (en) * 1996-02-20 1998-12-15 The United States Of America As Represented By The Department Of Health And Human Services Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II

Also Published As

Publication number Publication date
ID22177A (id) 1999-09-09
AU749658C (en) 2004-04-29
DK0951466T3 (da) 2009-03-16
SI0951466T1 (sl) 2009-10-31
HRP970705A2 (en) 1998-10-31
EA199900593A1 (ru) 2000-02-28
NO993098D0 (no) 1999-06-22
ATE421509T1 (de) 2009-02-15
EP0951466B1 (en) 2009-01-21
EA002100B1 (ru) 2001-12-24
CA2272305A1 (en) 1998-07-02
NZ335583A (en) 2001-03-30
AU749658B2 (en) 2002-06-27
HUP0001232A3 (en) 2001-02-28
JP3812952B2 (ja) 2006-08-23
NO993098L (no) 1999-08-20
ZA9711537B (en) 1998-06-25
PL196641B1 (pl) 2008-01-31
EP0951466A2 (en) 1999-10-27
PT951466E (pt) 2009-04-09
ES2319239T3 (es) 2009-05-05
JP2000511932A (ja) 2000-09-12
AR010854A1 (es) 2000-07-12
TR199901343T2 (xx) 1999-09-21
CN1242007A (zh) 2000-01-19
WO1998028268A2 (en) 1998-07-02
DE69739236D1 (de) 2009-03-12
WO1998028268A3 (en) 1998-10-08
AU5700798A (en) 1998-07-17
KR20000069654A (ko) 2000-11-25
CN1616432A (zh) 2005-05-18
IL129820A0 (en) 2000-02-29
CN1171878C (zh) 2004-10-20
HUP0001232A2 (hu) 2000-10-28
TW568914B (en) 2004-01-01
CO4930282A1 (es) 2000-06-27
PL334305A1 (en) 2000-02-14
IL158355A0 (en) 2004-05-12
BR9714517A (pt) 2000-07-04

Similar Documents

Publication Publication Date Title
PE52799A1 (es) Cicloalquilo, lactama, lactona y compuestos relacionados, composiciones farmaceuticas que comprenden los mismos, como inhibidores de la liberacion de peptido �-amiloide y no cicloalquilo, lactama, lactona y compuestos relacionados, como inhibidores de la liberacion del peptido �-amiloide
DE69100079D1 (de) Naphthalin-derivate, verfahren zu ihrer herstellung und sie enthaltende pharmazeutische zusammensetzungen.
FR2642968B1 (fr) Utilisation en cosmetique de diorganopolysiloxanes a fonction benzotriazole et nouvelles compositions cosmetiques contenant ces composes, destinees a la protection de la peau et des cheveux
PE57898A1 (es) Derivados de sulfonil urea
DK0738262T3 (da) Hidtil ukendte heterocykliske forbindelser
ES2112332T3 (es) Derivados de substitucion de oxigeno de productos de adicion de nucleofilo-oxido nitrico utilizados como promedicamentos donadores de oxido nitrico.
ES2102154T3 (es) Inhibicion de trombina.
PE46499A1 (es) Derivados de 6-fenilpiridil-2-amina
KR900006318A (ko) 피페리디닐 벤즈이미다졸
ES2177581T3 (es) Uso de compuestos de piperidina en el tratamiento de esquizofrenia.
AR029190A1 (es) Composiciones que contienen derivados del acido hidroxieicosatetraenoico y uso para la manufactura de un medicamento en el tratamiento de trastornos del ojo seco
NO901031L (no) Baktericid sammensetning.
DE3764885D1 (de) Neue 5-alkoxy-2,4-diamino-alkylbenzole sowie haarfaerbemittel mit 5-alkoxy-2,4-diamino-alkyl-benzolen.
ATE16805T1 (de) Trifluoromethylphenyltetrahydropyridine mit appetithemmender wirkung, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zusammensetzungen.
NO923265D0 (no) Benzol(f)quinolinoner
ATE150301T1 (de) Aminoalkanesulfonsäurederivate und pharmazeutische zusammensetzungen davon zur prävention oder behandlung von herzerkrankungen
DE59002863D1 (de) Lysolecithinderivate zur behandlung von autoimmunerkrankungen.
ES2098023T3 (es) Compuestos de estructura guanidinica y composiciones farmaceuticas que los contienen.
ES2043863T3 (es) Procedimiento para preparar derivados de la 1,2,5,6-tetrahidropiridina.
FR2713085B1 (fr) Composition tinctoriale contenant des p-phénylènediamines soufrées et procédés de teinture correspondants, nouvelles p-phénylènediamines soufrées et leur procédé de préparation.
DE69734764D1 (de) Eine amidgruppe tragende schwefelhaltige verbindungen, verfahren zu ihrer herstellung, deren verwendung in medikamenten und sie enthaltende pharmazeutische zubereitungen
FR2644696B1 (fr) Utilisation en cosmetique de diorganopolysiloxanes a fonction hydroxy-2 benzophenone et compositions cosmetiques contenant ces composes, destinees a la protection de la peau et des cheveux
ECSP941050A (es) Derivados de benzofurano, proceso para su preparacion y composicion farmaceutica que los contiene
ATE116647T1 (de) Thiophenderivate, verfahren zu deren herstellung und sie enthaltende pharmazeutische zusammensetzungen.
MX9300205A (es) Compuestos policiclicos disubstituidos y composicion farmaceutica que los contiene.

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed