DE60325968D1 - Prodrugs von exzitatorischen aminosäuren - Google Patents

Prodrugs von exzitatorischen aminosäuren

Info

Publication number
DE60325968D1
DE60325968D1 DE60325968T DE60325968T DE60325968D1 DE 60325968 D1 DE60325968 D1 DE 60325968D1 DE 60325968 T DE60325968 T DE 60325968T DE 60325968 T DE60325968 T DE 60325968T DE 60325968 D1 DE60325968 D1 DE 60325968D1
Authority
DE
Germany
Prior art keywords
prodrugs
amino acids
excitatory amino
excitatory
acids
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE60325968T
Other languages
German (de)
English (en)
Inventor
Eric David Moher
James Allen Monn
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of DE60325968D1 publication Critical patent/DE60325968D1/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • AIDS & HIV (AREA)
  • Ophthalmology & Optometry (AREA)
DE60325968T 2002-06-11 2003-06-06 Prodrugs von exzitatorischen aminosäuren Expired - Lifetime DE60325968D1 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP02380120 2002-06-11
EP02380121 2002-06-11
US41593602P 2002-10-03 2002-10-03
US41593702P 2002-10-03 2002-10-03
PCT/US2003/015405 WO2003104217A2 (en) 2002-06-01 2003-06-06 Prodrugs of excitatory amino acids

Publications (1)

Publication Number Publication Date
DE60325968D1 true DE60325968D1 (de) 2009-03-12

Family

ID=29740902

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60325968T Expired - Lifetime DE60325968D1 (de) 2002-06-11 2003-06-06 Prodrugs von exzitatorischen aminosäuren

Country Status (29)

Country Link
US (5) US7371872B2 (enExample)
EP (2) EP1897550A3 (enExample)
JP (2) JP4342437B2 (enExample)
KR (1) KR20080058509A (enExample)
AR (1) AR040257A1 (enExample)
AT (1) ATE421526T1 (enExample)
AU (1) AU2003232146B2 (enExample)
BR (1) BR0311558A (enExample)
CA (1) CA2488167C (enExample)
CO (1) CO5631438A2 (enExample)
CR (2) CR7616A (enExample)
CY (1) CY1108976T1 (enExample)
DE (1) DE60325968D1 (enExample)
DK (1) DK1517915T3 (enExample)
EA (2) EA011231B1 (enExample)
EC (1) ECSP085481A (enExample)
ES (1) ES2319116T3 (enExample)
HR (2) HRP20090058A2 (enExample)
IL (2) IL165100A0 (enExample)
MX (1) MXPA04012518A (enExample)
MY (1) MY146238A (enExample)
NO (2) NO331780B1 (enExample)
NZ (3) NZ564692A (enExample)
PE (1) PE20040555A1 (enExample)
PL (1) PL221489B1 (enExample)
PT (1) PT1517915E (enExample)
SI (1) SI1517915T1 (enExample)
WO (1) WO2003104217A2 (enExample)
ZA (1) ZA200409553B (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7371872B2 (en) * 2002-06-11 2008-05-13 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
MX2010002536A (es) 2007-09-14 2010-08-10 Ortho Mcneil Janssen Pharm 4-fenil-3,4,5,6-tetrahidro-2h, 1'h-[1,4]bipiridinil-2'-onas 1',3'-disubstituidas.
BRPI0918055A2 (pt) 2008-09-02 2015-12-01 Addex Pharmaceuticals Sa derivados de 3-azabiciclo[3,1,0]hexila como moduladores de receptores metabotrópicos de glutamato.
JP5656848B2 (ja) 2008-10-16 2015-01-21 ジャンセン ファーマシューティカルズ， インコーポレイテッド． 代謝型グルタミン酸受容体モジュレーターとしてのインドールおよびベンゾモルホリンの誘導体
CA2744138C (en) 2008-11-28 2015-08-11 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. 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
SG176021A1 (en) 2009-05-12 2011-12-29 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
ES2409006T3 (es) 2009-05-12 2013-06-24 Janssen Pharmaceuticals Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de los receptores mGluR2
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
AU2010266495B2 (en) * 2009-06-29 2013-10-03 Inolex Investment Corporation Non-petrochemically derived cationic emulsifiers that are neutralized amino acid esters and related compositions and methods
JO2978B1 (en) * 2009-12-21 2016-03-15 ايلي ليلي اند كومباني MGLU2 aids
US9012448B2 (en) 2010-11-08 2015-04-21 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
WO2012062759A1 (en) 2010-11-08 2012-05-18 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
AR083845A1 (es) * 2010-11-18 2013-03-27 Lilly Co Eli COMPUESTOS 3-FENILSULFANILMETIL-BICICLO[3.1.0]HEXANO 4-SUSTITUIDOS COMO ANTAGONISTAS DE mGluR2/3
KR101554793B1 (ko) * 2010-11-18 2015-09-21 일라이 릴리 앤드 캄파니 mGluR 2／3 길항제로서의 4-치환된-3-벤질옥시-비시클로［3.1.0］헥산 화합물
CA2836485C (en) * 2011-06-17 2016-12-13 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
NZ702237A (en) 2012-06-01 2016-08-26 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
PT3096790T (pt) 2014-01-21 2019-10-15 Janssen Pharmaceutica Nv Combinações compreendendo moduladores alostéricos positivos ou agonistas ortostéricos do recetor glutamatérgico metabotrópico do subtipo 2 e seu uso
EA202192105A3 (ru) 2014-02-04 2022-02-28 Янссен Фармацевтика Нв Комбинации, содержащие положительные аллостерические модуляторы или ортостерические агонисты метаботропного глутаматергического рецептора 2 подтипа, и их применение
CN105985389B (zh) * 2015-03-06 2019-03-19 北京大学 苯乙醇苷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
EP0732781B1 (fr) * 1995-03-14 2002-12-18 Brown & Sharpe Tesa S.A. Module comprenant une diode laser asservie et dispositif électro-optique muni d'un tel module
US5688826A (en) * 1995-11-16 1997-11-18 Eli Lilly And Company Excitatory amino acid derivatives
ZA969486B (en) * 1995-11-16 1998-05-12 Lilly Co Eli Excitatory amino acid derivatives.
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.
PT1052246E (pt) * 1998-01-28 2003-06-30 Taisho Pharmaceutical Co Ltd Derivados de amino-acidos contendo fluor
KR100469182B1 (ko) 1998-08-31 2005-02-02 다이쇼 세이야꾸 가부시끼가이샤 6-플루오로비시클로[3.1.0]헥산 유도체
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
WO2002000605A1 (en) * 2000-06-28 2002-01-03 Taisho Pharmaceutical Co., Ltd. Novel dicarboxylic acid derivatives
EP1351925A1 (en) * 2001-01-11 2003-10-15 Eli Lilly And Company Prodrugs of excitatory amino acids
CN1267407C (zh) * 2001-01-11 2006-08-02 伊莱利利公司 兴奋性氨基酸前体药物
US7067507B2 (en) * 2001-06-12 2006-06-27 Pharmacia & Upjohn Company Macrocycles useful in the treatment of Alzheimer's disease
CN1281274C (zh) * 2001-12-27 2006-10-25 大正制药株式会社 6－氟双环[3.1.0]己烷衍生物
WO2003084610A1 (en) * 2002-04-03 2003-10-16 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
US7371872B2 (en) 2002-06-11 2008-05-13 Eli Lilly And Company Prodrugs of excitatory amino acids

Also Published As

Publication number Publication date
KR20080058509A (ko) 2008-06-25
NO20050122L (no) 2005-01-10
HRP20041179A2 (en) 2005-06-30
EP1897550A3 (en) 2008-06-25
JP4342437B2 (ja) 2009-10-14
US7964632B2 (en) 2011-06-21
AU2003232146B2 (en) 2009-06-18
US7371872B2 (en) 2008-05-13
ES2319116T3 (es) 2009-05-04
PT1517915E (pt) 2009-04-09
NO20080765L (no) 2005-01-10
ZA200409553B (en) 2006-07-26
US20050222231A1 (en) 2005-10-06
HRP20041179B1 (hr) 2012-11-30
IL189355A0 (en) 2008-06-05
SI1517915T1 (sl) 2009-06-30
US7671082B2 (en) 2010-03-02
EA014979B1 (ru) 2011-04-29
IL189355A (en) 2014-05-28
AR040257A1 (es) 2005-03-23
NZ556437A (en) 2008-11-28
PL221489B1 (pl) 2016-04-29
EA200500007A1 (ru) 2006-06-30
ECSP085481A (es) 2008-05-30
EA200801711A1 (ru) 2008-12-30
CY1108976T1 (el) 2014-07-02
JP2008201779A (ja) 2008-09-04
HRP20090058A2 (hr) 2009-04-30
WO2003104217A2 (en) 2003-12-18
EP1897550A2 (en) 2008-03-12
AU2003232146A1 (en) 2003-12-22
BR0311558A (pt) 2007-04-27
NO331780B1 (no) 2012-03-26
MXPA04012518A (es) 2005-02-17
ATE421526T1 (de) 2009-02-15
US8153683B2 (en) 2012-04-10
WO2003104217A3 (en) 2004-02-26
US20120172422A1 (en) 2012-07-05
JP2006503807A (ja) 2006-02-02
EP1517915A2 (en) 2005-03-30
US20100113579A1 (en) 2010-05-06
CA2488167C (en) 2012-07-24
CR7616A (es) 2005-01-13
HK1075259A1 (en) 2005-12-09
IL165100A0 (en) 2005-12-18
MY146238A (en) 2012-07-31
EP1517915B1 (en) 2009-01-21
NZ564692A (en) 2009-05-31
US20080182889A1 (en) 2008-07-31
NZ536459A (en) 2008-03-28
CO5631438A2 (es) 2006-04-28
PL374381A1 (en) 2005-10-17
US20110207672A1 (en) 2011-08-25
CA2488167A1 (en) 2003-12-18
PE20040555A1 (es) 2004-08-30
EA011231B1 (ru) 2009-02-27
DK1517915T3 (da) 2009-03-16
CR20110130A (es) 2011-03-30

Similar Documents

Publication Publication Date Title
ATE421526T1 (de) Prodrugs von exzitatorischen aminosäuren
EP1501369A4 (en) PROTEIN PURIFICATION BASED ON NON AFFINITY
NO20054958D0 (no) Substitulerte aminokarboksylsyrer
DK1543038T4 (da) Proteinoprensning
DE60235619D1 (de) Kondensierte bizyklische oder trizyklische aminosäuren
NO20033078D0 (no) Hydrolysat av fiskeprotein
DE60328469D1 (de) Aminosäuren mit affinität zu alpha-2-delta-protein
DE60327407D1 (de) Immunmodulierende peptide
DE602004026242D1 (de) Derivate von alkalischen Aminosäuren als Geliermitteln
EP1578774A4 (en) PROTEIN PURIFICATION
NO20052807D0 (no) Fremgangsmate for fremstilling av aminosyrer
ATE356111T1 (de) Prodrugs von exzitatorischen aminosäuren
DE602004026773D1 (de) Verfahrensherstellung von ethern
IS2894B (is) Framleiðsla sómatóstatínpeptíða
EP1513959A4 (en) ANTIVIRAL INHIBITORS OF CAPSID PROTEINS
AU2002353845A1 (en) Prodrugs of excitatory amino acids
DE60215206D1 (de) Enzymatisches verfahren zur enantiomeren trennung von aminosäuren
TWI315666B (en) Prodrugs of excitatory amino acids
AU2003242924A1 (en) Prodrugs of excitatory amino acids
AU2002361611A1 (en) Prodrugs of excitatory amino acids
DE602004030633D1 (de) Reinigung von Amidderivaten
NO20053512D0 (no) IL-8-liknende proteiner
PT102827A (pt) Processo de producao n-(fosfonometil)glicina
NO20054532D0 (no) Fremgangsmater for a forhindre glukonoylering av proteiner
NO20050436D0 (no) Beta-lagnedbrytende peptider

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8328 Change in the person/name/address of the agent

Representative=s name: KROHER, STROBEL RECHTS- UND PATENTANWAELTE, 80336

8328 Change in the person/name/address of the agent

Representative=s name: DR. SCHOEN & PARTNER, 80336 MUENCHEN