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PE20140880A1 - Derivados de aminostatina para el tratamiento de artrosis - Google Patents

Derivados de aminostatina para el tratamiento de artrosis

Info

Publication number
PE20140880A1
PE20140880A1 PE2013001846A PE2013001846A PE20140880A1 PE 20140880 A1 PE20140880 A1 PE 20140880A1 PE 2013001846 A PE2013001846 A PE 2013001846A PE 2013001846 A PE2013001846 A PE 2013001846A PE 20140880 A1 PE20140880 A1 PE 20140880A1
Authority
PE
Peru
Prior art keywords
methyl
pentanoylamine
mono
substituted
aminostatine
Prior art date
Application number
PE2013001846A
Other languages
English (en)
Inventor
Markus Klein
Hans Guehring
Birgitta Leuthner
Christos Tsaklakidis
Original Assignee
Merck Patent Gmbh
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45464584&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140880(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of PE20140880A1 publication Critical patent/PE20140880A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1075—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of amino acids or peptide residues
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • 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
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • 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
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Analytical Chemistry (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE: I1, I2, I3, I4 E I5 SON INDEPENDIENTEMENTE N O CR�; R1 ES ALQUILO C1-10, NO SUSTITUIDO O MONO, DI, TRISUSTITUIDO CON =S, =NR, =O, ENTRE OTROS; A1 ES DE 0 A 4 RESTOS DE AMINOACIDOS UNIDOS ENTRE SI EN FORMA DE PEPTIDOS, CO, SO2, ENTRE OTROS; A2 ES DE 0 A 4 RESTOS DE AMINOACIDOS UNIDOS ENTRE SI EN FORMA DE PEPTIDOS; L1 ES UN ENLACE SIMPLE O CRR�; L2 ES UN ENLACE SIMPLE, CRR�, NR, ENTRE OTROS; X E Y SON H, FENILO O NAFTILO NO SUSTITUIDO O MONO, DI, TRI O TETRASUSTITUIDO CON R, ENTRE OTROS; R Y R� SON INDEPENDIENTEMENTE H, ALQUILO C1-10 NO SUSTITUIDO O MONO, DI, TRISUSTITUIDO CON =S, =NR, =O, ENTRE OTROS; m ES DE 0 A 4, n ES DE 0 A 2. ES UN COMPUESTO PREFERIDO: ESTER METILICO DEL ACIDO (S)-2-((2S,3S)-2-{(3S,4S)-3-AMINO-4-[(S)-2-((S)-2-TER-BUTOXICARBONILAMINO-4-METIL-PENTANOILAMINO)-BUTIRILAMINO]-5-FENIL-PENTANOILAMINO}-3-METIL-PENTANOILAMINO)-3-METIL-BUTIRICO; ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION
PE2013001846A 2011-02-08 2012-01-09 Derivados de aminostatina para el tratamiento de artrosis PE20140880A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11000974 2011-02-08

Publications (1)

Publication Number Publication Date
PE20140880A1 true PE20140880A1 (es) 2014-08-06

Family

ID=45464584

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013001846A PE20140880A1 (es) 2011-02-08 2012-01-09 Derivados de aminostatina para el tratamiento de artrosis

Country Status (21)

Country Link
US (2) US9345742B2 (es)
EP (1) EP2673287B1 (es)
JP (1) JP6326232B2 (es)
KR (1) KR20140053855A (es)
CN (1) CN103370331B (es)
AR (1) AR085332A1 (es)
AU (1) AU2012216230B2 (es)
BR (1) BR112013020025A2 (es)
CA (1) CA2826622C (es)
CL (1) CL2013002100A1 (es)
CO (1) CO6761336A2 (es)
EA (1) EA201300895A1 (es)
EC (1) ECSP13012868A (es)
ES (1) ES2649964T3 (es)
IL (1) IL227688B (es)
MX (1) MX2013009064A (es)
PE (1) PE20140880A1 (es)
PH (1) PH12013501368A1 (es)
SG (1) SG192592A1 (es)
TW (1) TW201309730A (es)
WO (1) WO2012107153A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105451754A (zh) * 2013-08-06 2016-03-30 默克专利股份有限公司 在关节病的情况下胃酶抑素的关节内施用
WO2019144805A1 (zh) * 2018-01-25 2019-08-01 四川科伦博泰生物医药股份有限公司 取代的苯乙胺化合物及其制备方法和用途

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4207554A (en) 1972-08-04 1980-06-10 Med-El Inc. Method and apparatus for automated classification and analysis of cells
US4125828A (en) 1972-08-04 1978-11-14 Med-El Inc. Method and apparatus for automated classification and analysis of cells
US3971736A (en) 1975-01-21 1976-07-27 Merck & Co., Inc. Cathepsin in D inhibitors
CA1258748A (en) 1981-10-08 1989-08-22 Daniel F. Veber Renin inhibitory peptides
DE3418491A1 (de) 1984-05-18 1985-11-21 Merck Patent Gmbh, 6100 Darmstadt Diaminosaeurederivate
CA1286846C (en) 1985-02-12 1991-07-23 Catherine Cazaubon Peptide derivatives which inhibit renin and acid proteases
DE3512128A1 (de) * 1985-04-03 1986-10-09 Merck Patent Gmbh, 6100 Darmstadt Peptide
DE3812328A1 (de) 1988-04-14 1989-10-26 Merck Patent Gmbh Aminosaeurederivate
US5378691A (en) * 1988-04-14 1995-01-03 Merck Patent Gesellschaft Mit Beschrankter Haftung Amino acid derivatives
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
US6150416A (en) 1997-02-04 2000-11-21 The Regents Of The University Of California Nanomolar, non-peptide inhibitors of cathepsin D
US5962506A (en) 1997-07-07 1999-10-05 Pharmacopeia, Inc. Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
US5986102A (en) 1998-04-29 1999-11-16 Pharmacopeia, Inc. Hydroxypropylamide peptidomimetics as inhibitors of aspartyl proteases
EP1515944A1 (en) 2002-06-17 2005-03-23 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
CN1863797A (zh) 2003-08-08 2006-11-15 先灵公司 具有苯甲酰胺取代基的环胺bace－1抑制剂
GB0325830D0 (en) 2003-11-05 2003-12-10 Novartis Ag Organic compounds
US20050261273A1 (en) 2004-03-09 2005-11-24 Varghese John Substituted urea and carbamate, phenacyl-2-hydroxy-3-diaminoalkane, and benzamide-2-hydroxy-3-diaminoalkane aspartyl-protease inhibitors
US20050239836A1 (en) 2004-03-09 2005-10-27 Varghese John Substituted hydroxyethylamine aspartyl protease inhibitors
GB0425569D0 (en) 2004-11-19 2004-12-22 Celltech R&D Ltd Biological products
RU2007130794A (ru) 2005-01-13 2009-02-20 Новартис АГ (CH) Макроциклические соединения для применения в качестве ингибиторов bace
US7812013B2 (en) 2005-06-14 2010-10-12 Schering Corporation Macrocyclic heterocyclic aspartyl protease inhibitors
US20070021400A1 (en) 2005-07-20 2007-01-25 Peter Herold Amino alcohols as therapeutic compounds
US20070021399A1 (en) 2005-07-20 2007-01-25 Peter Herold Amido-amino alcohols as therapeutic compounds
US20070021413A1 (en) 2005-07-20 2007-01-25 Peter Herold Diamino alcohols as therapeutic compounds
GB0526614D0 (en) 2005-12-30 2006-02-08 Novartis Ag Organic compounds
EP1872780A3 (en) 2006-06-14 2008-04-30 Speedel Experimenta AG Omega-Phenyloctanamides as therapeutic compounds
EP1867329A3 (en) 2006-06-14 2008-05-07 Speedel Experimenta AG 5-Amino-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamides as therapeutic compounds
GB0620729D0 (en) 2006-10-18 2006-11-29 Ucb Sa Biological products
EP1987834A3 (en) 2007-02-13 2008-11-19 Speedel Experimenta AG Substituted piperidines as therapeutic compounds
WO2008119772A1 (en) 2007-03-30 2008-10-09 Medivir Ab Amide derivatives as inhibitors of aspartyl proteases
WO2009013293A1 (en) 2007-07-24 2009-01-29 Novartis Ag Substituted cyclohexanecarboxamides useful as bace inhibitors
JP2011519911A (ja) 2008-05-05 2011-07-14 ノヴィミュンヌ エスア 抗ｉｌ１７ａ／ｉｌ−１７ｆ交差反応抗体及びその使用方法

Also Published As

Publication number Publication date
SG192592A1 (en) 2013-09-30
EP2673287B1 (de) 2017-08-30
US20130316955A1 (en) 2013-11-28
EA201300895A1 (ru) 2014-01-30
ES2649964T3 (es) 2018-01-16
JP2014510046A (ja) 2014-04-24
CL2013002100A1 (es) 2014-01-17
ECSP13012868A (es) 2013-10-31
TW201309730A (zh) 2013-03-01
BR112013020025A2 (pt) 2017-03-21
JP6326232B2 (ja) 2018-05-16
WO2012107153A1 (de) 2012-08-16
US9345742B2 (en) 2016-05-24
US20160228493A1 (en) 2016-08-11
US9839665B2 (en) 2017-12-12
IL227688B (en) 2019-08-29
AU2012216230A1 (en) 2013-09-19
AU2012216230B2 (en) 2017-05-25
MX2013009064A (es) 2013-10-01
PH12013501368A1 (en) 2013-08-28
CN103370331B (zh) 2017-02-15
KR20140053855A (ko) 2014-05-08
IL227688A0 (en) 2013-09-30
CA2826622C (en) 2021-03-02
EP2673287A1 (de) 2013-12-18
CN103370331A (zh) 2013-10-23
AR085332A1 (es) 2013-09-25
CO6761336A2 (es) 2013-09-30
CA2826622A1 (en) 2012-08-16

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