EA014979B1 - Пролекарства возбуждающих аминокислот - Google Patents

Пролекарства возбуждающих аминокислот Download PDF

Info

Publication number
EA014979B1
EA014979B1 EA200801711A EA200801711A EA014979B1 EA 014979 B1 EA014979 B1 EA 014979B1 EA 200801711 A EA200801711 A EA 200801711A EA 200801711 A EA200801711 A EA 200801711A EA 014979 B1 EA014979 B1 EA 014979B1
Authority
EA
Eurasian Patent Office
Prior art keywords
hexane
acid
mmol
tert
compound
Prior art date
Application number
EA200801711A
Other languages
English (en)
Russian (ru)
Other versions
EA200801711A1 (ru
Inventor
Эрик Дэвид Мохер
Джеймс Аллен Монн
Консепсьон Педрегал-Терсеро
Хаиме Гонзало Бланко-Ургоити
Иван Колладо Кано
Original Assignee
Эли Лилли Энд Компани
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 Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA200801711A1 publication Critical patent/EA200801711A1/ru
Publication of EA014979B1 publication Critical patent/EA014979B1/ru

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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • AIDS & HIV (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
EA200801711A 2002-06-11 2003-06-06 Пролекарства возбуждающих аминокислот EA014979B1 (ru)

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 (2)

Publication Number Publication Date
EA200801711A1 EA200801711A1 (ru) 2008-12-30
EA014979B1 true EA014979B1 (ru) 2011-04-29

Family

ID=29740902

Family Applications (2)

Application Number Title Priority Date Filing Date
EA200801711A EA014979B1 (ru) 2002-06-11 2003-06-06 Пролекарства возбуждающих аминокислот
EA200500007A EA011231B1 (ru) 2002-06-11 2003-06-06 Пролекарство возбуждающей аминокислоты и его применение

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA200500007A EA011231B1 (ru) 2002-06-11 2003-06-06 Пролекарство возбуждающей аминокислоты и его применение

Country Status (29)

Country Link
US (5) US7371872B2 (https=)
EP (2) EP1517915B1 (https=)
JP (2) JP4342437B2 (https=)
KR (1) KR20080058509A (https=)
AR (1) AR040257A1 (https=)
AT (1) ATE421526T1 (https=)
AU (1) AU2003232146B2 (https=)
BR (1) BR0311558A (https=)
CA (1) CA2488167C (https=)
CO (1) CO5631438A2 (https=)
CR (2) CR7616A (https=)
CY (1) CY1108976T1 (https=)
DE (1) DE60325968D1 (https=)
DK (1) DK1517915T3 (https=)
EA (2) EA014979B1 (https=)
EC (1) ECSP085481A (https=)
ES (1) ES2319116T3 (https=)
HR (2) HRP20090058A2 (https=)
IL (2) IL165100A0 (https=)
MX (1) MXPA04012518A (https=)
MY (1) MY146238A (https=)
NO (2) NO331780B1 (https=)
NZ (3) NZ564692A (https=)
PE (1) PE20040555A1 (https=)
PL (1) PL221489B1 (https=)
PT (1) PT1517915E (https=)
SI (1) SI1517915T1 (https=)
WO (1) WO2003104217A2 (https=)
ZA (1) ZA200409553B (https=)

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
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc １，４-二取代之３-氰基-吡啶酮衍生物及其作為ｍＧｌｕＲ２-受體之正向異位性調節劑之用途
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
PL2203439T3 (pl) 2007-09-14 2011-06-30 Addex Pharmaceuticals Sa 1',3'-dipodstawione-4-fenylo-3,4,5,6-tetrahydro-2H, 1'H-[1, 4']bipirydynylo-2'-ketony
JP5547194B2 (ja) 2008-09-02 2014-07-09 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の調節因子としての３−アザビシクロ［３．１．０］ヘキシル誘導体
RU2517181C2 (ru) 2008-10-16 2014-05-27 Орто-Макнейл-Янссен Фармасьютикалз, Инк. Производные индола и бензоморфолина в качестве модулятора метаботропных глутаматных рецепторов
WO2010060589A1 (en) 2008-11-28 2010-06-03 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
MY153912A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 1, 2, 4,-triazolo[4,3-a[pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
CN102439008B (zh) 2009-05-12 2015-04-29 杨森制药有限公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其用于治疗或预防神经和精神病症的用途
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
ES2837121T3 (es) * 2009-06-29 2021-06-29 Inolex Investment Corp Emulsionantes catiónicos derivados no petroquímicamente que son ésteres de aminoácidos neutralizados y composiciones y métodos relacionados
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
CN103261195B (zh) 2010-11-08 2015-09-02 杨森制药公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
EP2661435B1 (en) 2010-11-08 2015-08-19 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
CN103209954B (zh) * 2010-11-18 2015-09-02 伊莱利利公司 作为mGluR2/3拮抗剂的4-取代的-3-苄氧基-双环[3.1.0]己烷化合物
PT2721012T (pt) 2011-06-17 2016-07-27 Lilly Co Eli Derivados do ácido biciclo(3.1.0)hexano-2,6¿dicarboxílico como agonista do recetor mglu2
AR089718A1 (es) * 2012-02-01 2014-09-10 Lilly Co Eli AGONISTAS DE mGlu2/3
US9428483B2 (en) 2012-06-01 2016-08-30 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
KR20220049612A (ko) 2014-01-21 2022-04-21 얀센 파마슈티카 엔.브이. 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도
HUE053734T2 (hu) * 2014-01-21 2021-07-28 Janssen Pharmaceutica Nv 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait tartalmazó kombinációk és alkalmazásuk
CN108774274B (zh) * 2015-03-06 2020-11-03 北京大学 唾液酸甲酯甲苷衍生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

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993006127A1 (en) * 1991-09-17 1993-04-01 Warner-Lambert Company Novel amino acid prodrug renin inhibitors
US5688826A (en) * 1995-11-16 1997-11-18 Eli Lilly And Company Excitatory amino acid derivatives
WO1999038839A1 (en) * 1998-01-28 1999-08-05 Taisho Pharmaceutical Co., Ltd. Fluorine-containing amino acid derivatives
US5958960A (en) * 1997-05-14 1999-09-28 Eli Lilly And Company Excitatory amino acid receptor modulators
WO2000012464A1 (en) * 1998-08-31 2000-03-09 Taisho Pharmaceutical Co., Ltd. 6-fluorobicyclo[3. 1.0]hexane derivatives
WO2002000605A1 (en) * 2000-06-28 2002-01-03 Taisho Pharmaceutical Co., Ltd. Novel dicarboxylic acid derivatives
WO2002055485A1 (en) * 2001-01-11 2002-07-18 Eli Lilly And Company Prodrugs of excitatory amino acids
WO2002055481A1 (en) * 2001-01-11 2002-07-18 Eli Lilly And Company Prodrugs of excitatory amino acids
WO2003061698A1 (en) * 2001-12-27 2003-07-31 Taisho Pharmaceutical Co.,Ltd. 6-fluorobicyclo[3.1.0]hexane derivatives

Family Cites Families (12)

* 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
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
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
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
BR0210391A (pt) * 2001-06-12 2004-06-15 Elan Pharm Inc Composto, métodos de tratar um paciente que tenha ou de prevenir um paciente de contrair uma doença ou condição e de preparar um composto, e, uso de um composto
US20050192273A1 (en) * 2002-04-03 2005-09-01 Johnson Bryan G. Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist
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
EP1517915B1 (en) * 2002-06-11 2009-01-21 Eli Lilly And Company Prodrugs of excitatory amino acids

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993006127A1 (en) * 1991-09-17 1993-04-01 Warner-Lambert Company Novel amino acid prodrug renin inhibitors
US5688826A (en) * 1995-11-16 1997-11-18 Eli Lilly And Company Excitatory amino acid derivatives
US5958960A (en) * 1997-05-14 1999-09-28 Eli Lilly And Company Excitatory amino acid receptor modulators
WO1999038839A1 (en) * 1998-01-28 1999-08-05 Taisho Pharmaceutical Co., Ltd. Fluorine-containing amino acid derivatives
WO2000012464A1 (en) * 1998-08-31 2000-03-09 Taisho Pharmaceutical Co., Ltd. 6-fluorobicyclo[3. 1.0]hexane derivatives
WO2002000605A1 (en) * 2000-06-28 2002-01-03 Taisho Pharmaceutical Co., Ltd. Novel dicarboxylic acid derivatives
WO2002055485A1 (en) * 2001-01-11 2002-07-18 Eli Lilly And Company Prodrugs of excitatory amino acids
WO2002055481A1 (en) * 2001-01-11 2002-07-18 Eli Lilly And Company Prodrugs of excitatory amino acids
WO2003061698A1 (en) * 2001-12-27 2003-07-31 Taisho Pharmaceutical Co.,Ltd. 6-fluorobicyclo[3.1.0]hexane derivatives

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BRADSHAW TRACEY D. ET AL.: "Preclinical evaluation of amino acid prodrugs of novel antitumor 2-(4-amino-3-methylphenyl)benzothiazoles", MOLECULAR CANCER THERAPEUTICS, vol. 1, no. 4, February 2002 (2002-02), pages 239-246, XP009020684, ISSN: 1535-7163, the whole document *
OHSUMI K. ET AL.: "SYNTHESIS AND ANTITUMOR ACTIVITIES OF AMINO ACID PRODRUGS OF AMINO-COMBRETASTATINS", ANTI-CANCER DRUG DESIGN, BASINGSTOKE, GB, vol. 14, 1999, pages 539-548, XP002938076, ISSN: 0266-9536, the whole document *
SANCHEZ J.P. ET AL.: QUINOLONE ANTIBACTERIAL AGENTS. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF A SERIES OF AMINO ACID PRODRUGS OF RACEMIC AND CHIRAL 7-3-AMINO-1-PYRROLIDINYLQUINOLONES, HIGHLY SOLUBLE QUINOLONE PRODRUGS WITH IN VIVO PSEUDOMONAS ACTIVITY", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 35, no. 10, 15 May 1992 (1992-05-15), pages 1764-1773, XP001026653, ISSN: 0022-2623, the whole document *

Also Published As

Publication number Publication date
PE20040555A1 (es) 2004-08-30
JP2008201779A (ja) 2008-09-04
ES2319116T3 (es) 2009-05-04
EP1517915A2 (en) 2005-03-30
DK1517915T3 (da) 2009-03-16
EA200500007A1 (ru) 2006-06-30
EA011231B1 (ru) 2009-02-27
JP2006503807A (ja) 2006-02-02
AR040257A1 (es) 2005-03-23
NZ536459A (en) 2008-03-28
PL374381A1 (en) 2005-10-17
US20120172422A1 (en) 2012-07-05
ATE421526T1 (de) 2009-02-15
US7964632B2 (en) 2011-06-21
HRP20041179A2 (en) 2005-06-30
MY146238A (en) 2012-07-31
NZ564692A (en) 2009-05-31
EA200801711A1 (ru) 2008-12-30
CO5631438A2 (es) 2006-04-28
CA2488167C (en) 2012-07-24
CA2488167A1 (en) 2003-12-18
SI1517915T1 (sl) 2009-06-30
DE60325968D1 (de) 2009-03-12
BR0311558A (pt) 2007-04-27
HRP20090058A2 (hr) 2009-04-30
EP1897550A2 (en) 2008-03-12
ZA200409553B (en) 2006-07-26
HK1075259A1 (en) 2005-12-09
US8153683B2 (en) 2012-04-10
CR20110130A (es) 2011-03-30
KR20080058509A (ko) 2008-06-25
IL189355A (en) 2014-05-28
NZ556437A (en) 2008-11-28
WO2003104217A2 (en) 2003-12-18
EP1517915B1 (en) 2009-01-21
CY1108976T1 (el) 2014-07-02
JP4342437B2 (ja) 2009-10-14
US20050222231A1 (en) 2005-10-06
US20110207672A1 (en) 2011-08-25
PT1517915E (pt) 2009-04-09
AU2003232146A1 (en) 2003-12-22
AU2003232146B2 (en) 2009-06-18
EP1897550A3 (en) 2008-06-25
MXPA04012518A (es) 2005-02-17
IL165100A0 (en) 2005-12-18
ECSP085481A (es) 2008-05-30
HRP20041179B1 (hr) 2012-11-30
IL189355A0 (en) 2008-06-05
CR7616A (es) 2005-01-13
NO20080765L (no) 2005-01-10
US7371872B2 (en) 2008-05-13
NO331780B1 (no) 2012-03-26
US20100113579A1 (en) 2010-05-06
NO20050122L (no) 2005-01-10
US20080182889A1 (en) 2008-07-31
US7671082B2 (en) 2010-03-02
PL221489B1 (pl) 2016-04-29
WO2003104217A3 (en) 2004-02-26

Similar Documents

Publication Publication Date Title
EA014979B1 (ru) Пролекарства возбуждающих аминокислот
EP1368304B1 (en) Prodrugs of excitatory amino acids
CN100482680C (zh) 兴奋性氨基酸前药
AU2008200612B8 (en) Prodrugs of excitatory amino acids
PL221526B1 (pl) Związek o wzorze I, sposób jego wytwarzania, oraz jego zastosowanie w terapii
HK1116415A (en) Prodrugs of excitatory amino acids
RU2483077C2 (ru) Кристаллический d-изоглутамил-d-триптофан и моноаммонийная соль d-изоглутамил-d-триптофана
UA80280C2 (en) Prodrugs of excitatory amino acids
EP1310480A1 (en) Prodrugs of excitatory amino acids
HK1075259B (en) Prodrugs of excitatory amino acids

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM