AR040257A1 - Profarmacos de aminoacidos excitadores - Google Patents

Profarmacos de aminoacidos excitadores

Info

Publication number
AR040257A1
AR040257A1 ARP030102065A ARP030102065A AR040257A1 AR 040257 A1 AR040257 A1 AR 040257A1 AR P030102065 A ARP030102065 A AR P030102065A AR P030102065 A ARP030102065 A AR P030102065A AR 040257 A1 AR040257 A1 AR 040257A1
Authority
AR
Argentina
Prior art keywords
group
optionally substituted
aromatic
monocyclic
fluoro
Prior art date
Application number
ARP030102065A
Other languages
English (en)
Original Assignee
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR040257A1 publication Critical patent/AR040257A1/es

Links

Classifications

    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/555—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07C237/04—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 the carbon skeleton being acyclic and saturated
    • C07C237/12—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 the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • 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
    • 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
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07C2602/18—All rings being cycloaliphatic the ring system containing six carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

Se refiere a profármacos de aminoácidos excitadores sintéticos y a los procedimientos para su preparación. Se refiere además, a los procedimientos de uso, y a las composiciones farmacéuticas que comprenden, los compuestos para el tratamiento de trastornos neurológicos y trastornos siquiátricos. Reivindicación 1: Un compuesto de fórmula (1) en la que A es H-(Q)p-; Q se selecciona independientemente, tomado cada vez, del grupo aminoacilo; p es un número entero de 1 a 10; X es O, S; SO, SO2 o CR3R4; R3 es F, X´OR5, SO3H, tetrazolilo, CN, PO3R62, hidroxi, o NO2, N3, (CH2)mCOOR5a, (CH2)mPO3R6a2, NHCONHR5b, o NHSOR5c, R4 es H; o R3 y R4 juntos representan fluoro o R3 y R4 juntos representan =O, =NOR7, o =CR8R9, =CHCOOR5b, =CHPO3R6a2, o =CHCN; uno de R3 o R4 representa amino y el otro representa carboxilo; X´ representa un enlace CH2, o CO; m es un número entero de 1 a 3; R5, R5a, R5b, R5c, R7, R8, y R9 son independientemente un átomo de H; un grupo alquilo C1-6 opcionalmente sustituido; un grupo alquenilo C2-6 opcionalmente sustituido, un grupo alquinilo C2-6 opcionalmente sustituido, un grupo aromático opcionalmente sustituido, un grupo heteroaromático opcionalmente sustituido, un grupo carboxílico no aromático; un grupo heterocíclico no aromático; un grupo carboxílico monocíclico no aromático condensado con uno o dos grupos heteroaromáticos o aromáticos monocíclicos; o un grupo heterocíclico o monocíclico no aromático condensado con uno o dos grupos heteroaromáticos o aromáticos monocíclicos: R6 y R6a representan independientemente H o un grupo alquilo C1-6; R10 es H o fluoro; y R11 es H, fluoro o hidroxi; o una de sus sales farmacéuticamente aceptables.
ARP030102065A 2002-06-11 2003-06-10 Profarmacos de aminoacidos excitadores AR040257A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP02380120 2002-06-11
EP02380121 2002-06-11
US41593702P 2002-10-03 2002-10-03
US41593602P 2002-10-03 2002-10-03

Publications (1)

Publication Number Publication Date
AR040257A1 true AR040257A1 (es) 2005-03-23

Family

ID=29740902

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030102065A AR040257A1 (es) 2002-06-11 2003-06-10 Profarmacos de aminoacidos excitadores

Country Status (30)

Country Link
US (5) US7371872B2 (es)
EP (2) EP1517915B1 (es)
JP (2) JP4342437B2 (es)
KR (1) KR20080058509A (es)
AR (1) AR040257A1 (es)
AT (1) ATE421526T1 (es)
AU (1) AU2003232146B2 (es)
BR (1) BR0311558A (es)
CA (1) CA2488167C (es)
CO (1) CO5631438A2 (es)
CR (2) CR7616A (es)
CY (1) CY1108976T1 (es)
DE (1) DE60325968D1 (es)
DK (1) DK1517915T3 (es)
EA (2) EA011231B1 (es)
EC (1) ECSP085481A (es)
ES (1) ES2319116T3 (es)
HK (1) HK1075259A1 (es)
HR (2) HRP20041179B1 (es)
IL (2) IL165100A0 (es)
MX (1) MXPA04012518A (es)
MY (1) MY146238A (es)
NO (2) NO331780B1 (es)
NZ (3) NZ536459A (es)
PE (1) PE20040555A1 (es)
PL (1) PL221489B1 (es)
PT (1) PT1517915E (es)
SI (1) SI1517915T1 (es)
WO (1) WO2003104217A2 (es)
ZA (1) ZA200409553B (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1517915B1 (en) * 2002-06-11 2009-01-21 Eli Lilly And Company Prodrugs of excitatory amino acids
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
PT2203439E (pt) 2007-09-14 2011-02-11 Ortho Mcneil Janssen Pharm 4-fenil-3,4,5,6-tetra-hidro-2h,1'h-[1,4']bipiridinil-2'- onas 1',3'-dissubstituídas
RU2510396C2 (ru) 2008-09-02 2014-03-27 Янссен Фармасьютикалз, Инк. 3-азабицикло[3.1.0]гексильные производные в качестве модуляторов метаботропных глутаматных рецепторов
WO2010043396A1 (en) 2008-10-16 2010-04-22 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
AU2009319387B2 (en) 2008-11-28 2012-05-10 Addex Pharma S.A. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
WO2010111080A2 (en) 2009-03-27 2010-09-30 Eli Lilly And Company Optimized treatment of schizophrenia
NZ596078A (en) 2009-05-12 2013-06-28 Janssen Pharmaceuticals Inc 1,2,4-TRIAZOLO [4,3-a] PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
WO2010130422A1 (en) 2009-05-12 2010-11-18 Ortho-Mcneil-Janssen Pharmaceuticals, Inc 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
EP3300717B1 (en) * 2009-06-29 2020-09-23 Inolex Investment Corporation Non-petrochemically derived cationic emulsifiers that are neutralized amino acid esters and related compositions and methods
AR079343A1 (es) * 2009-12-21 2012-01-18 Lilly Co Eli Compuesto de acido 2-amino-4-(4h-1,2,4-triazol-3-ilsulfanil)biciclo[3.1.0]hexano-2,6-dicarboxilico, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar un trastorno psiquiatrico
US8993591B2 (en) 2010-11-08 2015-03-31 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a] pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
PL2649069T3 (pl) 2010-11-08 2016-01-29 Janssen Pharmaceuticals Inc Pochodne 1,2,4-triazolo[4,3-a]pirydyny i ich zastosowanie jako dodatnich allosterycznych modulatorów receptorów mGluR2
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
WO2012068041A1 (en) 2010-11-18 2012-05-24 Eli Lilly And Company 4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS
TWI520935B (zh) 2010-11-18 2016-02-11 美國禮來大藥廠 作為ｍＧｌｕＲ２／３拮抗劑之４－經取代－３－苯基磺醯基甲基－雙環［３.１.０］己烷化合物
AU2012271024B2 (en) 2011-06-17 2015-07-09 Eli Lilly And Company Bicyclo (3.1.0) hexane- 2, 6 -dicarboxylic acid derivatives as mGlu2 receptor agonist
AR089718A1 (es) * 2012-02-01 2014-09-10 Lilly Co Eli AGONISTAS DE mGlu2/3
MY169069A (en) 2012-06-01 2019-02-12 Taisho Pharmaceutical Co Ltd Prodrug of fluorine-containing amino acid
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
KR20200126026A (ko) 2014-01-21 2020-11-05 얀센 파마슈티카 엔.브이. 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도
EP3431106B1 (en) 2014-01-21 2020-12-30 Janssen Pharmaceutica NV Combinations comprising positive allosteric modulators of metabotropic glutamatergic receptor subtype 2 and their use
CN108752212B (zh) * 2015-03-06 2024-03-12 北京大学 9-脱羧迷迭香酸类似物及其合成方法和应用
JP6801835B2 (ja) 2015-07-09 2020-12-16 ミメトゲン ファーマシュウティカルズ インコーポレイテッドＭｉｍｅｔｏｇｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． β−ターンペプチド模倣環状塩の液相合成及び結晶化

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US200488A (en) 1878-02-19 Improvement in temporary binders
US1459765A (en) * 1922-03-18 1923-06-26 Wordsworth M Elliott Interchangeable sign letters
WO1993006127A1 (en) * 1991-09-17 1993-04-01 Warner-Lambert Company Novel amino acid prodrug renin inhibitors
US5849525A (en) 1994-03-09 1998-12-15 Brigham And Women's Hospital, Inc. Compositions corresponding to a proton-coupled peptide transporter and methods of making and using same
DE69529209T2 (de) * 1995-03-14 2003-11-13 Brown & Sharpe Tesa S.A., Renens Element mit einem geregelten Diodenlaser, und elektrooptische Vorrichtung unter Verwendung eines derartigen Elements
US5688826A (en) * 1995-11-16 1997-11-18 Eli Lilly And Company Excitatory amino acid derivatives
JP2000500748A (ja) * 1995-11-16 2000-01-25 イーライ・リリー・アンド・カンパニー 興奮性アミノ酸誘導体
US5952294A (en) 1996-07-31 1999-09-14 University Of Pittsburgh Of The Commonwealth System Of Higher Education Peptidyl prodrugs and methods of making and using the same
ZA983930B (en) * 1997-05-14 1999-11-08 Lilly Co Eli Excitatory amino acid receptor modulators.
AU734812B2 (en) * 1998-01-28 2001-06-21 Taisho Pharmaceutical Co., Ltd. Fluorine-containing amino acid derivatives
WO2000012464A1 (fr) * 1998-08-31 2000-03-09 Taisho Pharmaceutical Co., Ltd. Derives de 6-fluorobicyclo[3. 1.0]hexane
US6716452B1 (en) 2000-08-22 2004-04-06 New River Pharmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
US6313498B1 (en) * 1999-05-27 2001-11-06 Actrans System Inc. Flash memory cell with thin floating gate with rounded side wall, and fabrication process
KR20030017562A (ko) * 2000-06-28 2003-03-03 다이쇼 세이야꾸 가부시끼가이샤 신규 디카르복실산 유도체
EP1351925A1 (en) * 2001-01-11 2003-10-15 Eli Lilly And Company Prodrugs of excitatory amino acids
HUP0400620A3 (en) * 2001-01-11 2012-09-28 Lilly Co Eli Prodrugs of excitatory amino acids and pharmaceutical compositions containing them and process for preparation the compounds
US7067507B2 (en) * 2001-06-12 2006-06-27 Pharmacia & Upjohn Company Macrocycles useful in the treatment of Alzheimer's disease
KR20090031962A (ko) 2001-12-27 2009-03-30 다이쇼 세이야꾸 가부시끼가이샤 6-플루오로비시클로[3.1.0]헥산 유도체
AU2003218063A1 (en) * 2002-04-03 2003-10-20 Eli Lilly And Company Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist
US20050192273A1 (en) * 2002-04-03 2005-09-01 Johnson Bryan G. Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist
EP1517915B1 (en) * 2002-06-11 2009-01-21 Eli Lilly And Company Prodrugs of excitatory amino acids

Also Published As

Publication number Publication date
JP4342437B2 (ja) 2009-10-14
US20110207672A1 (en) 2011-08-25
US20100113579A1 (en) 2010-05-06
EA200801711A1 (ru) 2008-12-30
US20120172422A1 (en) 2012-07-05
CY1108976T1 (el) 2014-07-02
PL374381A1 (en) 2005-10-17
MXPA04012518A (es) 2005-02-17
NZ556437A (en) 2008-11-28
IL189355A (en) 2014-05-28
HRP20090058A2 (en) 2009-04-30
US7671082B2 (en) 2010-03-02
US7371872B2 (en) 2008-05-13
EA014979B1 (ru) 2011-04-29
CR7616A (es) 2005-01-13
KR20080058509A (ko) 2008-06-25
AU2003232146B2 (en) 2009-06-18
US7964632B2 (en) 2011-06-21
MY146238A (en) 2012-07-31
ES2319116T3 (es) 2009-05-04
CR20110130A (es) 2011-03-30
JP2008201779A (ja) 2008-09-04
HRP20041179B1 (hr) 2012-11-30
IL189355A0 (en) 2008-06-05
CA2488167C (en) 2012-07-24
WO2003104217A3 (en) 2004-02-26
EP1517915A2 (en) 2005-03-30
HK1075259A1 (en) 2005-12-09
EP1897550A3 (en) 2008-06-25
EP1897550A2 (en) 2008-03-12
JP2006503807A (ja) 2006-02-02
CA2488167A1 (en) 2003-12-18
EA011231B1 (ru) 2009-02-27
NO20050122L (no) 2005-01-10
ATE421526T1 (de) 2009-02-15
NO331780B1 (no) 2012-03-26
US20080182889A1 (en) 2008-07-31
SI1517915T1 (sl) 2009-06-30
NZ536459A (en) 2008-03-28
EA200500007A1 (ru) 2006-06-30
EP1517915B1 (en) 2009-01-21
PT1517915E (pt) 2009-04-09
AU2003232146A1 (en) 2003-12-22
DE60325968D1 (de) 2009-03-12
NO20080765L (no) 2005-01-10
DK1517915T3 (da) 2009-03-16
WO2003104217A2 (en) 2003-12-18
HRP20041179A2 (en) 2005-06-30
CO5631438A2 (es) 2006-04-28
US20050222231A1 (en) 2005-10-06
PL221489B1 (pl) 2016-04-29
US8153683B2 (en) 2012-04-10
BR0311558A (pt) 2007-04-27
ZA200409553B (en) 2006-07-26
NZ564692A (en) 2009-05-31
IL165100A0 (en) 2005-12-18
PE20040555A1 (es) 2004-08-30
ECSP085481A (es) 2008-05-30

Similar Documents

Publication Publication Date Title
AR040257A1 (es) Profarmacos de aminoacidos excitadores
AR109033A2 (es) Derivados de 1,4-benzotiepina-1,1-dióxido sustituidos con radicales bencilo, productos farmacéuticos que comprenden estos compuestos y su uso
AR054125A1 (es) Derivados del fluoreno, composiciones farmaceuticas que los contienen y su utilizacion en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la actividad de la proteina hsp90
AR062677A1 (es) Derivados de biaril-sulfonamida, procesos de produccion y composiciones farmaceuticas que los comprenden
CY1106679T1 (el) Αζαδικυκλικες ετεροκυκλικες ενωσεις ως τροποποιητες κανναβινοειδους υποδοχεα
CO5580820A2 (es) Derivados novedosos de acido (2s)-3-(4-{2-[amino]-2-oxoetoxi} fenil)-2-etoxipropanoico procesos para su preparacion y composiciones farmaceuticas que los contienen
AR033678A1 (es) Derivados de quinolina, procedimiento para prepararlos, uso de los mismos para la preparacion de medicamentos y los medicamentos que contienen dichos derivados
AR048834A1 (es) Compuestos derivados de piperidina o tropano; metodos para su preparacion; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por quimioquinas (ccr5)
CY1109227T1 (el) Παραγωγα της 5-φαινυλο-4-μεθυλο-θειαζολ-2-υλ-αμινης ως αναστολεις των ενζυμων κινασης της φωσφατιδυλινοσιτολης 3 (p13) για την θεραπεια των φλεγμονωδων ασθενειων των αεραγωγων
AR025386A1 (es) Moduladores de los receptores activados del proliferador de peroxisomas
TR200103337T2 (tr) Protez inhibit”rleri olarak yeni bileçikler ve bileçimler
FI962749A0 (fi) Uusia heterosyklisiä yhdisteitä
AR051771A1 (es) Acidos amino carboxilicos sustituidos
AR058180A1 (es) Indeno derivados, su preparacion y su uso como medicamentos
AR048567A1 (es) Derivados de benzoxazinona, su preparacion y composiciones farmaceuticas.
CO2022001853A2 (es) Derivados de 2-morfolinopiridina sustituidos como inhibidores de la cinasa atr
DK529888A (da) Substituerede n-(1-alkyl-3-hydroxy-4-piperidinyl) benzamider
AR034241A1 (es) Compuestos que inhiben carboxipeptidasas, un proceso para su preparacion, una formulacion farmaceutica que los contiene y uso de los mismos para la fabricacion de un medicamento
SE0101579D0 (sv) New compounds
AR059030A1 (es) Combinacion de derivados de triazina y estimuladores de la secrecion de insulina
AR045793A1 (es) Compuestos derivados de 3-heterociclil-indol
AR013462A1 (es) Nuevos peptidomimeticos para el tratamiento de trastornos oseos, metodos para su produccion y drogas que contienen estos compuestos
AR045950A1 (es) Compuestos derivados de piperazina, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos.
EA200300272A1 (ru) Новые производные хиназолина, способ их получения и фармацевтические композиции, содержащие их
DK1257552T3 (da) Xanthinderivater, mellemprodukter og anvendelse til behandling af osteoporose

Legal Events

Date Code Title Description
FG Grant, registration
FG Grant, registration