ZA9711537B - Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds. - Google Patents

Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds.

Info

Publication number
ZA9711537B
ZA9711537B ZA9711537A ZA9711537A ZA9711537B ZA 9711537 B ZA9711537 B ZA 9711537B ZA 9711537 A ZA9711537 A ZA 9711537A ZA 9711537 A ZA9711537 A ZA 9711537A ZA 9711537 B ZA9711537 B ZA 9711537B
Authority
ZA
South Africa
Prior art keywords
compounds
lactam
lactone
cycloalkyl
inhibiting
Prior art date
Application number
ZA9711537A
Other languages
English (en)
Inventor
Jing Wu
Jay S Tung
Eugene D Thorsett
Michael A Pleiss
Jeffrey S Nissen
Jeffrey Neitz
Lee H Latimer
Varghese John
Stephen Freedman
Thomas C Britton
James E Audia
Jon K Reel
Thomas E Mabry
Bruce A Dressman
Cynthia L Cwi
James J Droste
Steven S Henry
Stacey L Mcdaniel
William Leonard Scott
Russell D Stucky
Warren J Porter
Original Assignee
Athena Neurosciences Inc Eli L
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 Eli L filed Critical Athena Neurosciences Inc Eli L
Publication of ZA9711537B publication Critical patent/ZA9711537B/xx

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)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (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)
ZA9711537A 1996-12-23 1997-12-22 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds. ZA9711537B (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ZA9711537B true ZA9711537B (en) 1998-06-25

Family

ID=25118329

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA9711537A ZA9711537B (en) 1996-12-23 1997-12-22 Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds.

Country Status (28)

Country Link
EP (1) EP0951466B1 (xx)
JP (1) JP3812952B2 (xx)
KR (1) KR20000069654A (xx)
CN (2) CN1171878C (xx)
AR (1) AR010854A1 (xx)
AT (1) ATE421509T1 (xx)
AU (1) AU749658C (xx)
BR (1) BR9714517A (xx)
CA (1) CA2272305A1 (xx)
CO (1) CO4930282A1 (xx)
DE (1) DE69739236D1 (xx)
DK (1) DK0951466T3 (xx)
EA (1) EA002100B1 (xx)
ES (1) ES2319239T3 (xx)
HR (1) HRP970705A2 (xx)
HU (1) HUP0001232A3 (xx)
ID (1) ID22177A (xx)
IL (2) IL158355A0 (xx)
NO (1) NO993098L (xx)
NZ (1) NZ335583A (xx)
PE (1) PE52799A1 (xx)
PL (1) PL196641B1 (xx)
PT (1) PT951466E (xx)
SI (1) SI0951466T1 (xx)
TR (1) TR199901343T2 (xx)
TW (1) TW568914B (xx)
WO (1) WO1998028268A2 (xx)
ZA (1) ZA9711537B (xx)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20010033408A (ko) * 1997-12-22 2001-04-25 진 엠. 듀발 폴리시클릭 α-아미노-ε-카프롤락탐 및 관련 화합물
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
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
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
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
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
WO2000038618A2 (en) 1998-12-24 2000-07-06 Du Pont Pharmaceuticals Company SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
AU6071400A (en) * 1999-07-06 2001-01-22 Vertex Pharmaceuticals Incorporated Cyclized amide derivatives
AU6420700A (en) * 1999-08-05 2001-03-05 Prescient Neuropharma Inc. Novel 1,4-benzodiazepine compounds and derivatives thereof
US6503902B2 (en) 1999-09-13 2003-01-07 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of a β protein production
MXPA02001813A (es) 1999-09-13 2004-03-19 Bristol Myers Squibb Pharma Co Hidroxialcanoilaminolactamas y estructuras relacionas como inhibidores de la produccion de la proteina abeta.
US6960576B2 (en) 1999-09-13 2005-11-01 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
EP1222176A1 (en) 1999-10-08 2002-07-17 Bristol-Myers Squibb Pharma Company AMINO LACTAM SULFONAMIDES AS INHIBITORS OF A$g(b) PROTEIN PRODUCTION
WO2001034571A1 (en) * 1999-11-09 2001-05-17 Eli Lilly And Company β-AMINOACID COMPOUNDS USEFUL FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS
AU2001239791A1 (en) 2000-02-17 2001-08-27 Du Pont Pharmaceuticals Company Succinoylamino carbocycles and heterocycles as inhibitors of abeta protein production
US6495540B2 (en) 2000-03-28 2002-12-17 Bristol - Myers Squibb Pharma Company Lactams as inhibitors of A-β protein production
EP1267906A1 (en) * 2000-03-28 2003-01-02 Bristol-Myers Squibb Pharma Company 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
MXPA02009755A (es) 2000-04-03 2003-03-27 Bristol Myers Squibb Pharma Co Lactamas ciclicas como inhibidores de la produccion de proteina a-beta.
CA2404273A1 (en) 2000-04-11 2001-10-18 Bristol-Myers Squibb Pharma Company Substituted lactams as inhibitors of a.beta. protein production
WO2001087354A2 (en) 2000-05-17 2001-11-22 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
AU783857B2 (en) 2000-06-01 2005-12-15 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
US7468365B2 (en) 2000-11-17 2008-12-23 Eli Lilly And Company Lactam compound
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
AU2002224322A1 (en) * 2000-11-17 2002-05-27 Eli Lilly And Company Lactam dipeptide and its use in inhibiting beta-amyloid peptiderelease
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
PT1362052E (pt) 2001-01-17 2007-04-30 Amura Therapeutics Ltd Inibidores de cruzipaína e de outras proteases de cisteína
JP2004520365A (ja) 2001-01-17 2004-07-08 アミュラ テラピューティクス リミテッド クルジパインおよび他のシステインプロテアーゼの阻害剤
CA2435117A1 (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
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
AU2003276201A1 (en) * 2002-11-11 2004-06-03 Bayer Healthcare Ag Phenyl or heteroaryl amino alkane derivatives as ip receptor antagonist
ATE496893T1 (de) 2002-12-20 2011-02-15 X Ceptor Therapeutics Inc Isochinolinonderivate und deren verwendung als medikamente
FR2850380B1 (fr) * 2003-01-23 2006-07-07 Sanofi Synthelabo Derives d'acylaminothiazole, leur preparation et leur utilisation en therapeutique
EP1636196A1 (en) * 2003-03-14 2006-03-22 AstraZeneca AB Novel lactams and uses thereof
WO2004098589A1 (en) 2003-05-02 2004-11-18 Elan Pharmaceuticals, Inc. 4- bromo - 5 - (2- chloro - benzoylamino) - 1h - pyrazole - 3 - carboxylic acid amide derivatives and related compounds as bradykinin b1 receptor antagonists for the treatment of inflammatory diseases
ITMI20032278A1 (it) 2003-11-21 2005-05-22 Ethicon Endo Surgery Inc Dispositivo di diagnosi
PL1691814T3 (pl) * 2003-12-01 2012-12-31 Cambridge Entpr Ltd Środki przeciwzapalne
CA2556436C (en) 2004-02-23 2014-04-01 Eli Lilly And Company Process for preparing anti-a.beta. antibody
AU2005287137B2 (en) 2004-09-17 2012-03-22 Foldrx Pharmaceuticals, Inc. 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
AU2007334260A1 (en) 2006-11-15 2008-06-26 Massachusetts Eye & Ear Infirmary Generation of inner ear cells
WO2008099210A2 (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
WO2009023453A1 (en) 2007-08-14 2009-02-19 Eli Lilly And Company Azepine derivatives as gamma-secretase inhibitors
DK2222636T3 (da) 2007-12-21 2013-06-03 Ligand Pharm Inc Selektive androgenreceptormodulatorer (SARMS) og anvendelser deraf
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
WO2010060088A2 (en) 2008-11-24 2010-05-27 Massachusetts Eye & Ear Infirmary Pathways to generate hair cells
WO2010084979A1 (en) * 2009-01-23 2010-07-29 Banyu Pharmaceutical Co.,Ltd. Benzodiazepin-2-on derivatives
AU2010216632A1 (en) * 2009-02-17 2011-08-04 Msd K.K. 1,4-benzodiazepin-2-on derivatives
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
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. 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
EP2721031B1 (en) 2011-06-17 2016-01-20 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
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
WO2014039781A1 (en) 2012-09-07 2014-03-13 Massachusetts Eye & Ear Infirmary 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
EP3094323A4 (en) 2014-01-17 2017-10-11 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
EP3157928B1 (en) 2014-06-20 2019-02-13 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
US20170314027A1 (en) 2014-08-06 2017-11-02 Massachusetts Eye And Ear Infirmary Increasing atoh1 life to drive sensorineural hair cell differentiantion
WO2016025681A1 (en) 2014-08-13 2016-02-18 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
CN109219439B (zh) 2016-01-29 2022-09-20 马萨诸塞眼科耳科诊所 内耳支持细胞的扩增和分化及其使用方法
WO2017180389A1 (en) 2016-04-12 2017-10-19 Eli Lilly And Company Combination therapy with notch and cdk4/6 inhibitors for the treatment of cancer
CN109310685B (zh) 2016-04-12 2021-10-29 伊莱利利公司 用于治疗癌症的notch和pi3k/mtor抑制剂的组合疗法
CN109689071B (zh) 2016-05-16 2023-05-30 通用医疗公司 肺上皮工程中的人气道干细胞
CN115845070A (zh) 2016-05-20 2023-03-28 伊莱利利公司 用notch和pd-1或pd-l1抑制剂的组合治疗
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
US11376259B2 (en) 2016-10-12 2022-07-05 Eli Lilly And Company Targeted treatment of mature T-cell lymphoma
KR20190098998A (ko) 2016-12-16 2019-08-23 파이프라인 테라퓨틱스, 아이엔씨. 달팽이관 시냅스질환의 치료 방법
CN110461335A (zh) 2017-02-17 2019-11-15 弗雷德哈钦森癌症研究中心 用于治疗bcma相关癌症和自身免疫性失调的联合疗法
EP3743057A4 (en) 2018-01-26 2021-11-17 Massachusetts Eye & 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
IE42215B1 (en) * 1973-12-28 1980-07-02 Fujisawa Pharmaceutical Co Azetidinone derivatives and process for preparation thereof
FR2278335A1 (fr) * 1974-07-04 1976-02-13 Fujisawa Pharmaceutical Co Derives d'azetidinones et leurs procedes de preparation
ZA945719B (en) * 1993-08-09 1996-02-01 Lilly Co Eli Identification and use of protease inhibitors
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
EP0951466A2 (en) 1999-10-27
AU749658B2 (en) 2002-06-27
EP0951466B1 (en) 2009-01-21
CN1242007A (zh) 2000-01-19
PL196641B1 (pl) 2008-01-31
DK0951466T3 (da) 2009-03-16
WO1998028268A3 (en) 1998-10-08
IL129820A0 (en) 2000-02-29
TR199901343T2 (xx) 1999-09-21
CA2272305A1 (en) 1998-07-02
BR9714517A (pt) 2000-07-04
EA002100B1 (ru) 2001-12-24
EA199900593A1 (ru) 2000-02-28
DE69739236D1 (de) 2009-03-12
HRP970705A2 (en) 1998-10-31
SI0951466T1 (sl) 2009-10-31
AU749658C (en) 2004-04-29
TW568914B (en) 2004-01-01
ES2319239T3 (es) 2009-05-05
NO993098L (no) 1999-08-20
JP2000511932A (ja) 2000-09-12
IL158355A0 (en) 2004-05-12
AU5700798A (en) 1998-07-17
CN1171878C (zh) 2004-10-20
ATE421509T1 (de) 2009-02-15
JP3812952B2 (ja) 2006-08-23
HUP0001232A2 (hu) 2000-10-28
NO993098D0 (no) 1999-06-22
PL334305A1 (en) 2000-02-14
HUP0001232A3 (en) 2001-02-28
PT951466E (pt) 2009-04-09
CO4930282A1 (es) 2000-06-27
CN1616432A (zh) 2005-05-18
KR20000069654A (ko) 2000-11-25
ID22177A (id) 1999-09-09
AR010854A1 (es) 2000-07-12
PE52799A1 (es) 1999-05-27
WO1998028268A2 (en) 1998-07-02
NZ335583A (en) 2001-03-30

Similar Documents

Publication Publication Date Title
ZA9711537B (en) Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds.
ZA981627B (en) Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds.
HUP0100270A3 (en) Peptids for inhibiting betha-amyloid peptide release and/or its synthesis, pharmaceutical compositions comprising thereof and their use
HUP9901199A3 (en) Tropane-derivatives, inhibiting neurotransmitter re-uptake, their preparation, pharmaceutical compositions containing them and use of the compounds
HUP9901159A3 (en) Substituted benzylaminopiperidine derivatives and use thereof, pharmaceutical compositions containing these compounds
CY2369B1 (en) Substituted heterocyclic compounds, preparation method therefor and pharmaceutical compositions containing same.
HUP0100601A3 (en) Bicyclic compounds containing nitrogen, processes for their preparation and pharmaceutical compositions thereof
EP1093372A4 (en) CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHODS OF INHIBITING PEPTIDE RELEASE $ g (b) -AMYLOID AND / OR ITS SYNTHESIS USING THE SAME
HK1002384A1 (en) Pharmaceutical compositions containing irbesartan
HUP9902455A3 (en) 6-phenylpyridyl-2-amine derivatives, pharmaceutical compositions containing them
HUP0000492A3 (en) N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
HUP0001652A3 (en) Oxadiazole derivatives, processes for their preparation, their use and pharmaceutical compositions containing them
WO2002047671A3 (en) Lactam compound to inhibit beta-amyloid peptide release or synthesis
EP1037639A4 (en) HETEROARYL-SUBSTITUTED IMIDAZOLE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS AND USES
IL133420A0 (en) Pharmaceutical composition for combination of piperidinoalkanol-decongestant
HUP0103913A3 (en) Novel form of irbesartan, methods for obtaining said form and pharmaceutical compositions containing same
HRP960558B1 (en) New crystalline modifications of cdch, processes for the preparation thereof and pharmaceutical compositions containing them
HK1028352A1 (en) Solid pharmaceutical composition containing benzofurane derivatives.
HUP0003851A3 (en) Pharmaceutical composition for the treatment or prevention of glomerulopathy
IL109703A0 (en) Substituted carbazole derivatives, processes for their preparation and pharmaceutical compositions containing them
IL123094A0 (en) Pharmaceutical compositions containing griseofulvin for inhibiting the growth of cancers
HUP9901326A3 (en) Benzopyran derivatives having leukotriene-antagonistic action, pharmaceutical compositions containing these compounds, process for the preparation and use of these compounds and compositions
ZA9710272B (en) Pharmaceutical compositions comprising diaryl-cyclomethylenpyrazole compounds.
HUP9901189A3 (en) Peptide derivatives,which inhibit t-cell activation, process for producing them and pharmaceutical compositions containing them
HUP9603001A3 (en) Heterocycle compounds comprising nitrogen, process for producing them and pharmaceutical compositions containing the same