PE38997A1 - TACHYCININE ANTAGONIST - Google Patents

TACHYCININE ANTAGONIST

Info

Publication number
PE38997A1
PE38997A1 PE1995286859A PE28685995A PE38997A1 PE 38997 A1 PE38997 A1 PE 38997A1 PE 1995286859 A PE1995286859 A PE 1995286859A PE 28685995 A PE28685995 A PE 28685995A PE 38997 A1 PE38997 A1 PE 38997A1
Authority
PE
Peru
Prior art keywords
phenyl
compound
formula
disstituted
carbamoil
Prior art date
Application number
PE1995286859A
Other languages
Spanish (es)
Inventor
Soo Young Ko
Christopher Walpole
Original Assignee
Novartis Ag
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
Priority claimed from GBGB9425085.9A external-priority patent/GB9425085D0/en
Priority claimed from GBGB9426016.3A external-priority patent/GB9426016D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE38997A1 publication Critical patent/PE38997A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof

Landscapes

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

Abstract

SE REFIERE AL COMPUESTO ANALGESICO Y ANTIINFLAMATORIO DE FORMULA I DONDE: R1 ES FENILO MONO O DISUSTITUIDO POR UNO O DOS MIEMBROS SELECCIONADOS DE HALOGENO, NITRO, CIANO ENTRE OTROS; n ES CERO O UNO; X1 ES OXIGENO, AZUFRE o =NCN; X2 Y X3 SON CADA UNO INDEPENDIENTEMENTE OXIGENO O AZUFRE; R2 ES HIDROGENO O METILO; R3 ES FENILO, FENILO SUSTITUIDO CON HALO, 2-NAFTILO, ENTRE OTROS; Z ES -N(CH3) o -CH2-; R4 ES FENILO, 3,5-BIS(TRIFLUOROMETIL)FENILO O PIRIDILO; R5 ES HIDROGENO, FENILO, 3,5-BIS(TRIFLUOROMETIL)FENILO O PIRIDILO; TAMBIEN SE REFIERE AL PROCESO DE PRODUCCION QUE COMPRENDE LA REACCION DEL COMPUESTO DE FORMULA II DONDE R2, R3, R4 Y R5 YA SE DEFINIERON, CON EL COMPUESTO DE FORMULA R1`-(CH2)n-N=C=X1 EN LA QUE R1' ES FENILO, MONO O DISUSTITUIDO POR UNO O DOS MIEMBROS SELECCIONADOS DEL GRUPO QUE CONSISTE DE HALOGENO, NITRO, CIANO ENTRE OTROS; n Y X1 TIENEN LOS SIGNIFICADOS YA INDICADOS; CUANDO SE REQUIERE, LLEVAR A CABO LA DESPROTECCION DEL COMPUESTO ASI OBTENIDO, EN EL QUE R1' ES FENILO SUSTITUIDO POR HIDROXI PROTEGIDO Y/O HIDROXIMETILO PROTEGIDO Y/O REALIZAR LA TRANSFORMACION DEL COMPUESTO ASI OBTENIDO, EN EL QUE R1 ES FENILO SUSTITUIDO POR METOXICARBONILO, PARA OBTENER EL COMPUESTO CORRESPONDIENTE EN EL QUE R1' ES FENILO SUSTITUIDO POR CARBAMOILO o N-METILCARBAMOILO Y LUEGO LA RECUPERACION DEL COMPUESTOIT REFERS TO THE ANALGESIC AND ANTI-INFLAMMATORY COMPOUND OF FORMULA I WHERE: R1 IS MONO PHENYLUS OR DISSTITUTED BY ONE OR TWO SELECTED MEMBERS OF HALOGEN, NITRO, CIANO AMONG OTHERS; n IS ZERO OR ONE; X1 IS OXYGEN, SULFUR, or = NCN; X2 AND X3 ARE EACH INDEPENDENTLY OXYGEN OR SULFUR; R2 IS HYDROGEN OR METHYL; R3 IS PHENYL, PHENYL SUBSTITUTED WITH HALO, 2-NAPHTHYL, AMONG OTHERS; Z IS -N (CH3) or -CH2-; R4 IS PHENYL, 3,5-BIS (TRIFLUOROMETHYL) PHENYL OR PIRIDYL; R5 IS HYDROGEN, PHENYL, 3,5-BIS (TRIFLUOROMETIL) PHENYL OR PIRIDYL; IT ALSO REFERS TO THE PRODUCTION PROCESS THAT INCLUDES THE REACTION OF THE COMPOUND OF FORMULA II WHERE R2, R3, R4 AND R5 HAVE ALREADY BEEN DEFINED, WITH THE COMPOUND OF FORMULA R1`- (CH2) nN = C = X1 WHERE R1 'IS FENILE, MONKEY OR DISSTITUTED BY ONE OR TWO SELECTED MEMBERS OF THE GROUP THAT CONSISTS OF HALOGEN, NITRO, CIANO AMONG OTHERS; n AND X1 HAVE THE MEANINGS ALREADY INDICATED; WHEN REQUIRED, CARRY OUT THE DEPROTECTION OF THE COMPOUND SO OBTAINED, IN WHICH R1 'IS PHENYL SUBSTITUTED FOR PROTECTED HYDROXY AND / OR HYDROXYMETHYLUM PROTECTED AND / OR PERFORM THE ESOOIL, ENOIL , TO OBTAIN THE CORRESPONDING COMPOUND IN WHICH R1 'IS PHENYL SUBSTITUTED BY CARBAMOIL OR N-METHYL CARBAMOIL AND THEN RECOVERY OF THE COMPOUND

PE1995286859A 1994-12-13 1995-12-11 TACHYCININE ANTAGONIST PE38997A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9425085.9A GB9425085D0 (en) 1994-12-13 1994-12-13 Organic compounds
GBGB9426016.3A GB9426016D0 (en) 1994-12-22 1994-12-22 Organic compounds

Publications (1)

Publication Number Publication Date
PE38997A1 true PE38997A1 (en) 1997-10-02

Family

ID=26306161

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1995286859A PE38997A1 (en) 1994-12-13 1995-12-11 TACHYCININE ANTAGONIST

Country Status (17)

Country Link
EP (1) EP0797583A1 (en)
JP (1) JPH10511935A (en)
AR (1) AR001332A1 (en)
AU (1) AU4343796A (en)
BR (1) BR9509997A (en)
CA (1) CA2204130A1 (en)
CO (1) CO4700289A1 (en)
CZ (1) CZ179097A3 (en)
FI (1) FI971685A7 (en)
HU (1) HUT77002A (en)
IL (1) IL116323A0 (en)
NO (1) NO972526D0 (en)
PE (1) PE38997A1 (en)
PL (1) PL320217A1 (en)
SK (1) SK74697A3 (en)
TR (1) TR199501568A2 (en)
WO (1) WO1996018643A1 (en)

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DE69736390T2 (en) * 1996-10-07 2007-07-26 Merck Sharp & Dohme Ltd., Hoddesdon CNS PENETRATING NK-1 RECEPTOR ANTAGONISTS AS ANTIDEPRESSIVE AND / OR ANXIOLYTIC
JP2002542151A (en) 1999-02-18 2002-12-10 科研製薬株式会社 Novel amide derivatives as growth hormone secretagogues
MXPA02004330A (en) 1999-11-03 2004-07-30 Albany Molecular Res Inc Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin.
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
KR100821410B1 (en) 2000-07-11 2008-04-10 에이엠알 테크놀로지, 인크. 4-phenyl substituted tetrahydroisoquinoline and its therapeutic use
NZ552397A (en) 2004-07-15 2011-04-29 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
ES2382814T3 (en) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Cis-4 - [(4-chlorophenyl) sulfonyl] -4- (2,5-difluorophenyl) cyclohexanopropanoic acid for cancer treatment
KR101594898B1 (en) 2005-07-15 2016-02-18 알바니 몰레큘라 리써치, 인크. Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
EP1940842B1 (en) 2005-09-29 2012-05-30 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
US8173629B2 (en) 2006-09-22 2012-05-08 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
JP4611444B2 (en) 2007-01-10 2011-01-12 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー Amide substituted indazoles as poly (ADP-ribose) polymerase (PARP) inhibitors
EP2117538A1 (en) 2007-01-24 2009-11-18 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
JP5319518B2 (en) 2007-04-02 2013-10-16 Msd株式会社 Indoledione derivative
AU2008269154B2 (en) 2007-06-27 2014-06-12 Merck Sharp & Dohme Llc 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
AU2009222122A1 (en) 2008-03-03 2009-09-11 Tiger Pharmatech Tyrosine kinase inhibitors
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
WO2010132437A1 (en) 2009-05-12 2010-11-18 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
AU2010247763B2 (en) 2009-05-12 2015-12-24 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
AU2010247735B2 (en) 2009-05-12 2015-07-16 Albany Molecular Research, Inc. Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydroisoquinoline and use thereof
PE20121172A1 (en) 2009-10-14 2012-09-05 Merck Sharp & Dohme PIPERIDINS SUBSTITUTED WITH ACTIVITY IN HDM2
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
EP3330377A1 (en) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
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US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
AU2012245971A1 (en) 2011-04-21 2013-10-17 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
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KR102196882B1 (en) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Substituted imidazopyridines as hdm2 inhibitors
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EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
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US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors

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JPH05186498A (en) * 1991-12-27 1993-07-27 Japan Tobacco Inc Proline derivative

Also Published As

Publication number Publication date
EP0797583A1 (en) 1997-10-01
AU4343796A (en) 1996-07-03
WO1996018643A1 (en) 1996-06-20
FI971685L (en) 1997-08-13
MX9703957A (en) 1997-09-30
TR199501568A2 (en) 1996-07-21
CZ179097A3 (en) 1997-10-15
FI971685A0 (en) 1997-04-18
PL320217A1 (en) 1997-09-15
BR9509997A (en) 1997-12-30
FI971685A7 (en) 1997-08-13
IL116323A0 (en) 1996-03-31
HUT77002A (en) 1998-03-02
SK74697A3 (en) 1997-11-05
CO4700289A1 (en) 1998-12-29
JPH10511935A (en) 1998-11-17
CA2204130A1 (en) 1996-06-20
AR001332A1 (en) 1997-10-22
NO972526L (en) 1997-06-03
NO972526D0 (en) 1997-06-03

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