ATE421526T1 - Prodrugs von exzitatorischen aminosäuren - Google Patents

Prodrugs von exzitatorischen aminosäuren

Info

Publication number
ATE421526T1
ATE421526T1 AT03757266T AT03757266T ATE421526T1 AT E421526 T1 ATE421526 T1 AT E421526T1 AT 03757266 T AT03757266 T AT 03757266T AT 03757266 T AT03757266 T AT 03757266T AT E421526 T1 ATE421526 T1 AT E421526T1
Authority
AT
Austria
Prior art keywords
prodrugs
amino acids
excitatory amino
excitatory
acids
Prior art date
Application number
AT03757266T
Other languages
English (en)
Inventor
Eric Moher
James Monn
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
Application granted granted Critical
Publication of ATE421526T1 publication Critical patent/ATE421526T1/de

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
    • 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
    • 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
    • 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)
  • 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)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
AT03757266T 2002-06-11 2003-06-06 Prodrugs von exzitatorischen aminosäuren ATE421526T1 (de)

Applications Claiming Priority (4)

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

Publications (1)

Publication Number Publication Date
ATE421526T1 true ATE421526T1 (de) 2009-02-15

Family

ID=29740902

Family Applications (1)

Application Number Title Priority Date Filing Date
AT03757266T ATE421526T1 (de) 2002-06-11 2003-06-06 Prodrugs von exzitatorischen aminosäuren

Country Status (29)

Country Link
US (5) US7371872B2 (de)
EP (2) EP1897550A3 (de)
JP (2) JP4342437B2 (de)
KR (1) KR20080058509A (de)
AR (1) AR040257A1 (de)
AT (1) ATE421526T1 (de)
AU (1) AU2003232146B2 (de)
BR (1) BR0311558A (de)
CA (1) CA2488167C (de)
CO (1) CO5631438A2 (de)
CR (2) CR7616A (de)
CY (1) CY1108976T1 (de)
DE (1) DE60325968D1 (de)
DK (1) DK1517915T3 (de)
EA (2) EA014979B1 (de)
EC (1) ECSP085481A (de)
ES (1) ES2319116T3 (de)
HR (2) HRP20041179B1 (de)
IL (2) IL165100A0 (de)
MX (1) MXPA04012518A (de)
MY (1) MY146238A (de)
NO (2) NO331780B1 (de)
NZ (3) NZ556437A (de)
PE (1) PE20040555A1 (de)
PL (1) PL221489B1 (de)
PT (1) PT1517915E (de)
SI (1) SI1517915T1 (de)
WO (1) WO2003104217A2 (de)
ZA (1) ZA200409553B (de)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20041179B1 (hr) * 2002-06-11 2012-11-30 Eli Lilly And Company Prekursorski oblici lijekova za aminokiseline s pobuđivačkom aktivnosti
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
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
EA017648B1 (ru) 2007-09-14 2013-02-28 Орто-Макнейл-Янссен Фармасьютикалз, Инк. 1',3'-двузамещенные-4-фенил-3,4,5,6-тетрагидро-2н,1'н-[1,4']бипириди-нил-2'-оны
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
WO2010043396A1 (en) 2008-10-16 2010-04-22 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
JP5690277B2 (ja) 2008-11-28 2015-03-25 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インドールおよびベンゾオキサジン誘導体
WO2010111080A2 (en) 2009-03-27 2010-09-30 Eli Lilly And Company Optimized treatment of schizophrenia
HRP20131122T1 (hr) 2009-05-12 2013-12-20 Janssen Pharmaceuticals, Inc. Derivati 1,2,4-triazolo[4,3-a] piridina i njihova uporaba u lijeäśenju ili prevenciji neuroloških i psihijatrijskih poremeä†aja
CN102439015B (zh) 2009-05-12 2015-05-13 杨森制药有限公司 1,2,4-三唑并[4,3-a]吡啶衍生物和其作为mGluR2受体的正向变构调节剂的用途
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
CN102549138B (zh) * 2009-06-29 2015-04-01 伊诺莱克斯投资公司 不含石化衍生中性氨基酸酯的阳离子型乳化剂及其组合物和方法
JO2978B1 (en) * 2009-12-21 2016-03-15 ايلي ليلي اند كومباني MGLU2 aids
ES2536433T3 (es) 2010-11-08 2015-05-25 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
EP2661435B1 (de) 2010-11-08 2015-08-19 Janssen Pharmaceuticals, Inc. 1,2,4-triazol[4,3-a]pyridinderivate und ihre verwendung als positive allosterische mglur2-rezeptormodulatoren
JP5852664B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド １，２，４−トリアゾロ［４，３−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
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
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
KR101598679B1 (ko) * 2011-06-17 2016-02-29 일라이 릴리 앤드 캄파니 mGlu2 수용체 효능제로서의 비시클로(3.1.0)헥산-2,6-디카르복실산 유도체
AR089718A1 (es) * 2012-02-01 2014-09-10 Lilly Co Eli AGONISTAS DE mGlu2/3
EP2857385B1 (de) 2012-06-01 2017-08-02 Taisho Pharmaceutical Co., Ltd. Prodrug aus fluorhaltiger aminosäure
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
PL3096790T3 (pl) * 2014-01-21 2020-01-31 Janssen Pharmaceutica, N.V. Kombinacje zawierające pozytywne modulatory allosteryczne lub agonistów ortosterycznych metabotropowego receptora glutaminergicznego podtypu 2 i ich zastosowanie
ME03518B (de) * 2014-01-21 2020-04-20 Janssen Pharmaceutica Nv Kombinationen mit positiven allosterischen modulatoren von metabotropem glutamatergen rezeptor vom subtyp 2 und deren verwendung
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
KR102056257B1 (ko) 2015-07-09 2019-12-16 미메토젠 파르마슈티칼스 인크. 베타-턴 펩티도미메틱 사이클릭 염의 용액상 합성 및 결정화

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
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
US5688826A (en) * 1995-11-16 1997-11-18 Eli Lilly And Company 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.
CN1182105C (zh) * 1998-01-28 2004-12-29 大正制药株式会社 含氟氨基酸衍生物
DE69918136T2 (de) * 1998-08-31 2005-07-07 Taisho Pharmaceutical Co., Ltd. 6-Fluorobicyclo[3.1.0]Hexan-Derivate
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
CN1216038C (zh) * 2000-06-28 2005-08-24 大正制药株式会社 新型二羧酸衍生物
WO2002055485A1 (en) * 2001-01-11 2002-07-18 Eli Lilly And Company Prodrugs of excitatory amino acids
US7256217B2 (en) * 2001-01-11 2007-08-14 Eli Lilly And Company Prodrugs of excitatory amino acids
EP1395257A1 (de) * 2001-06-12 2004-03-10 Elan Pharmaceuticals, Inc. Makrocyclische verbindungen zur behandlung der alzheimer-krankheit
PL208123B1 (pl) * 2001-12-27 2011-03-31 Taisho Pharmaceutical Co Ltd Pochodna kwasu 2-amino-3-alkoksy-6-fluorobicyklo [3.1.0] heksano-2, 6-dikarboksylowego, zawierająca ją kompozycja farmaceutyczna i lek, oraz jej zastosowanie
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
HRP20041179B1 (hr) * 2002-06-11 2012-11-30 Eli Lilly And Company Prekursorski oblici lijekova za aminokiseline s pobuđivačkom aktivnosti

Also Published As

Publication number Publication date
EP1897550A2 (de) 2008-03-12
MXPA04012518A (es) 2005-02-17
NZ564692A (en) 2009-05-31
US20110207672A1 (en) 2011-08-25
SI1517915T1 (sl) 2009-06-30
DE60325968D1 (de) 2009-03-12
NZ556437A (en) 2008-11-28
DK1517915T3 (da) 2009-03-16
ES2319116T3 (es) 2009-05-04
US20080182889A1 (en) 2008-07-31
MY146238A (en) 2012-07-31
US7371872B2 (en) 2008-05-13
HRP20041179B1 (hr) 2012-11-30
IL189355A0 (en) 2008-06-05
IL189355A (en) 2014-05-28
US8153683B2 (en) 2012-04-10
US20050222231A1 (en) 2005-10-06
AR040257A1 (es) 2005-03-23
EA014979B1 (ru) 2011-04-29
CY1108976T1 (el) 2014-07-02
JP4342437B2 (ja) 2009-10-14
ZA200409553B (en) 2006-07-26
KR20080058509A (ko) 2008-06-25
US20100113579A1 (en) 2010-05-06
US7671082B2 (en) 2010-03-02
ECSP085481A (es) 2008-05-30
US7964632B2 (en) 2011-06-21
EA200801711A1 (ru) 2008-12-30
HK1075259A1 (en) 2005-12-09
CR20110130A (es) 2011-03-30
EP1897550A3 (de) 2008-06-25
EA011231B1 (ru) 2009-02-27
WO2003104217A2 (en) 2003-12-18
US20120172422A1 (en) 2012-07-05
CO5631438A2 (es) 2006-04-28
PL221489B1 (pl) 2016-04-29
EP1517915A2 (de) 2005-03-30
NO20080765L (no) 2005-01-10
NO20050122L (no) 2005-01-10
JP2006503807A (ja) 2006-02-02
WO2003104217A3 (en) 2004-02-26
CA2488167A1 (en) 2003-12-18
CA2488167C (en) 2012-07-24
AU2003232146A1 (en) 2003-12-22
PL374381A1 (en) 2005-10-17
HRP20041179A2 (en) 2005-06-30
AU2003232146B2 (en) 2009-06-18
EP1517915B1 (de) 2009-01-21
PE20040555A1 (es) 2004-08-30
NO331780B1 (no) 2012-03-26
NZ536459A (en) 2008-03-28
JP2008201779A (ja) 2008-09-04
EA200500007A1 (ru) 2006-06-30
HRP20090058A2 (hr) 2009-04-30
CR7616A (es) 2005-01-13
PT1517915E (pt) 2009-04-09
BR0311558A (pt) 2007-04-27
IL165100A0 (en) 2005-12-18

Similar Documents

Publication Publication Date Title
DE60325968D1 (de) Prodrugs von exzitatorischen aminosäuren
NO20054958D0 (no) Substitulerte aminokarboksylsyrer
DK1543038T4 (da) Proteinoprensning
EP1514106A4 (de) Gezielte therapeutische proteine
DE60235619D1 (de) Kondensierte bizyklische oder trizyklische aminosäuren
EP1625208A4 (de) Neues lipolytisches enzym lip2
NO20033078L (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 (de) Proteinaufreinigung
DE602004015504D1 (de) Von injektionspräparaten
DE60127182D1 (de) Prodrugs von exzitatorischen aminosäuren
DE602004026773D1 (de) Verfahrensherstellung von ethern
DE50313548D1 (de) Zerstäubungsanordnung
EP1513959A4 (de) Antivirale inhibitoren von capsidproteinen
IS8338A (is) Framleiðsla sómatóstatínpeptíða
AU2002353845A1 (en) Prodrugs of excitatory amino acids
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
NO20054532D0 (no) Fremgangsmater for a forhindre glukonoylering av proteiner
NO20053512D0 (no) IL-8-liknende proteiner
PT102827B (pt) Processo de producao n-(fosfonometil)glicina

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 1517915

Country of ref document: EP