PE20141680A1 - Agonistas de mglu 2/3 - Google Patents

Agonistas de mglu 2/3

Info

Publication number
PE20141680A1
PE20141680A1 PE2014001210A PE2014001210A PE20141680A1 PE 20141680 A1 PE20141680 A1 PE 20141680A1 PE 2014001210 A PE2014001210 A PE 2014001210A PE 2014001210 A PE2014001210 A PE 2014001210A PE 20141680 A1 PE20141680 A1 PE 20141680A1
Authority
PE
Peru
Prior art keywords
bicycle
hexane
agonists
compounds
aminopropanoyl
Prior art date
Application number
PE2014001210A
Other languages
English (en)
Inventor
Stephen Richard Baker
Christopher David Beadle
Barry Peter Clark
James Allen Monn
Lourdes Prieto
Original Assignee
Lilly Co Eli
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20141680A1 publication Critical patent/PE20141680A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/26—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms containing rings other than aromatic rings
    • C07C55/30—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms containing rings other than aromatic rings containing condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C229/50—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms being part of the same condensed ring 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
    • 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
    • A61P25/18—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
    • A61P25/22—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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/52—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/753—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring of polycyclic acids
    • 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
    • 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
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/93—Spiro compounds
    • C07C2603/94—Spiro compounds containing "free" spiro atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE BICICLO[3.1.0]HEXANO 4-SUSTITUIDO DE FORMULA (I) DONDE R1 Y R3 SON CADA UNO H, BENCILO O (2-FLUOROFENIL)METILO; R2 ES H, (2S)-2-AMINOPROPANOILO, (2S)-2-AMINO-4-METILSULFANIL-BUTANOIL, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO (1S,2S,5R,6S)-2-AMINOESPIRO[BICICLO[3.1.0]HEXANO-4,1'-CICLOPROPANO]-2,6-DICARBOXILICO; ACIDO (1S,2S,5R,6S)-2-[[(2S)-2-AMINOPROPANOIL]AMINO]ESPIRO[BICICLO[3.1.0]HEXANO-4,1'-CICLOPROPANO]-2,6-DICARBOXILICO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON AGONISTAS DE RECEPTORES DE GLUTAMATO METABOTROPICO MGLU2/3 SIENDO UTILES EN EL TRATAMIENTO DE DOLOR NEUROPATICO, ESQUIZOFRENIA, TRASTORNO BIPOLAR
PE2014001210A 2012-02-01 2013-01-29 Agonistas de mglu 2/3 PE20141680A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12382038 2012-02-01
US201261619139P 2012-04-02 2012-04-02

Publications (1)

Publication Number Publication Date
PE20141680A1 true PE20141680A1 (es) 2014-11-08

Family

ID=48870759

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014001210A PE20141680A1 (es) 2012-02-01 2013-01-29 Agonistas de mglu 2/3

Country Status (35)

Country Link
US (1) US8575214B2 (es)
EP (1) EP2809647B1 (es)
JP (1) JP5755821B2 (es)
KR (1) KR101518365B1 (es)
CN (1) CN104093703B (es)
AP (1) AP2014007821A0 (es)
AR (1) AR089718A1 (es)
AU (1) AU2013215396B2 (es)
BR (1) BR112014018760A8 (es)
CA (1) CA2863085C (es)
CL (1) CL2014001928A1 (es)
CO (1) CO7020921A2 (es)
CR (1) CR20140344A (es)
DK (1) DK2809647T3 (es)
DO (1) DOP2014000179A (es)
EA (1) EA023678B1 (es)
ES (1) ES2592166T3 (es)
GT (1) GT201400168A (es)
HK (1) HK1199014A1 (es)
HR (1) HRP20160867T1 (es)
HU (1) HUE028863T2 (es)
IL (1) IL233732A0 (es)
LT (1) LT2809647T (es)
MA (1) MA35884B1 (es)
MX (1) MX355779B (es)
NZ (1) NZ626456A (es)
PE (1) PE20141680A1 (es)
PH (1) PH12014501725A1 (es)
PL (1) PL2809647T3 (es)
PT (1) PT2809647T (es)
RS (1) RS54976B1 (es)
SG (1) SG11201404138VA (es)
SI (1) SI2809647T1 (es)
TW (1) TW201343610A (es)
WO (1) WO2013116174A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101481164B1 (ko) * 2008-01-30 2015-01-09 주식회사 미래셀바이오 체세포 유래 다능성 줄기세포의 제조 방법

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9605429D0 (en) * 1995-11-16 1996-05-15 Lilly Co Eli Excitatory amino acid receptor antagonists
PL326695A1 (en) 1995-11-16 1998-10-26 Lilly Co Eli Derivatives of stimulating aminoacids
ZA983930B (en) 1997-05-14 1999-11-08 Lilly Co Eli Excitatory amino acid receptor modulators.
US6333428B1 (en) * 1998-08-31 2001-12-25 Taisho Pharmaceutical Co., Ltd. 6-fluorobicyclo[3.1.0]hexane derivatives
GB2355982A (en) * 1999-11-03 2001-05-09 Lilly Co Eli Heterocyclic amino acids
EP1295865A4 (en) * 2000-06-28 2005-06-01 Taisho Pharmaceutical Co Ltd NEW DICARBOXYLENE DERIVATIVES
WO2002055485A1 (en) 2001-01-11 2002-07-18 Eli Lilly And Company Prodrugs of excitatory amino acids
HUP0400620A3 (en) 2001-01-11 2012-09-28 Lilly Co Eli Prodrugs of excitatory amino acids and pharmaceutical compositions containing them and process for preparation the compounds
KR20080058509A (ko) 2002-06-11 2008-06-25 일라이 릴리 앤드 캄파니 흥분성 아미노산의 전구약물
NZ544131A (en) 2003-06-26 2009-11-27 Taisho Pharmaceutical Co Ltd 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative
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

Also Published As

Publication number Publication date
EA201491291A1 (ru) 2014-10-30
JP5755821B2 (ja) 2015-07-29
EP2809647A1 (en) 2014-12-10
CL2014001928A1 (es) 2014-11-07
IL233732A0 (en) 2014-09-30
CA2863085A1 (en) 2013-08-08
AR089718A1 (es) 2014-09-10
ES2592166T3 (es) 2016-11-28
PT2809647T (pt) 2016-08-29
AP2014007821A0 (en) 2014-07-31
SI2809647T1 (sl) 2016-08-31
CN104093703B (zh) 2016-01-20
AU2013215396A1 (en) 2014-07-17
MX2014008598A (es) 2014-08-22
AU2013215396B2 (en) 2015-03-12
AU2013215396A8 (en) 2014-08-07
CO7020921A2 (es) 2014-08-11
DK2809647T3 (en) 2016-10-03
MA35884B1 (fr) 2014-12-01
US20130197079A1 (en) 2013-08-01
BR112014018760A8 (pt) 2017-07-11
MX355779B (es) 2018-04-30
NZ626456A (en) 2016-02-26
BR112014018760A2 (es) 2017-06-20
CN104093703A (zh) 2014-10-08
EP2809647B1 (en) 2016-07-06
DOP2014000179A (es) 2014-10-15
KR20140107658A (ko) 2014-09-04
RS54976B1 (sr) 2016-11-30
JP2015512870A (ja) 2015-04-30
CA2863085C (en) 2015-11-17
HUE028863T2 (en) 2017-01-30
HRP20160867T1 (hr) 2016-10-07
GT201400168A (es) 2015-08-27
WO2013116174A1 (en) 2013-08-08
PL2809647T3 (pl) 2017-07-31
HK1199014A1 (en) 2015-06-19
KR101518365B1 (ko) 2015-05-08
LT2809647T (lt) 2016-10-10
PH12014501725A1 (en) 2014-11-24
CR20140344A (es) 2014-08-25
EA023678B1 (ru) 2016-06-30
US8575214B2 (en) 2013-11-05
SG11201404138VA (en) 2014-08-28
TW201343610A (zh) 2013-11-01

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