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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic 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
    • C07D411/12—Heterocyclic 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
    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof

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) FI971685A (en)
HU (1) HUT77002A (en)
IL (1) IL116323A0 (en)
NO (1) NO972526L (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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JP2001502311A (en) * 1996-10-07 2001-02-20 メルク シヤープ エンド ドーム リミテツド CNS permeable NK-1 receptor antagonist as antidepressant and / or anxiolytic
EP1158996A4 (en) 1999-02-18 2005-01-12 Kaken Pharma Co Ltd Novel amide derivatives as growth hormone secretagogues
GEP20094640B (en) 2004-07-15 2009-03-10 Bristol Myers Squibb Co Aryl-and heteroaryl-substituted tetrahydro isoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
ATE550019T1 (en) 2005-05-17 2012-04-15 Merck Sharp & Dohme CIS-4-Ä(4-CHLOROPHENYL)SULFONYLÜ-4-(2,5-DIFLUOROPHENYL)CYCLOHEXANEPROPANE ACID FOR THE TREATMENT OF CANCER
BRPI0613403A2 (en) 2005-07-15 2009-02-10 Amr Technology Inc aryl and heteroaryl substituted tetrahydrobenzodiazepines and their use to block reuptake of norepinephrine, dopamine and serotonin
CA2624030A1 (en) 2005-09-29 2007-04-12 Tianying Jian Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2083831B1 (en) 2006-09-22 2013-12-25 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-)
EP2145884B1 (en) 2007-04-02 2014-08-06 Msd K.K. Indoledione derivative
US8389553B2 (en) 2007-06-27 2013-03-05 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
JP2011515343A (en) 2008-03-03 2011-05-19 タイガー ファーマテック Tyrosine kinase inhibitor
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
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
KR101830447B1 (en) 2009-05-12 2018-02-20 알바니 몰레큘라 리써치, 인크. 7-([1,2,4]TRIAZOLO[1,5-α]PYRIDIN-6-YL)-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDROISOQUINOLINE AND USE THEREOF
JP5739415B2 (en) 2009-05-12 2015-06-24 ブリストル−マイヤーズ スクウィブ カンパニー (S) -7-([1,2,4] triazolo [1,5-a] pyridin-6-yl) -4- (3,4-dichlorophenyl) -1,2,3,4-tetrahydroisoquinoline Crystal forms and uses thereof
EP2429295B1 (en) 2009-05-12 2013-12-25 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
CN102638981B (en) 2009-10-14 2015-07-22 默沙东公司 Substituted piperidines that increase p53 activity and the uses thereof
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
EP2606134B1 (en) 2010-08-17 2019-04-10 Sirna Therapeutics, Inc. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
EP2632472B1 (en) 2010-10-29 2017-12-13 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
JP2014514321A (en) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション Insulin-like growth factor 1 receptor inhibitor
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
EP3453762B1 (en) 2012-05-02 2021-04-21 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
US9233979B2 (en) 2012-09-28 2016-01-12 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
RU2660349C2 (en) 2012-11-28 2018-07-05 Мерк Шарп И Доум Корп. Compositions and methods for treatment of malignant tumour
BR112015013611A2 (en) 2012-12-20 2017-11-14 Merck Sharp & Dohme compound and pharmaceutical composition
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
EP3706742B1 (en) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. 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
WO1996018643A1 (en) 1996-06-20
IL116323A0 (en) 1996-03-31
FI971685A (en) 1997-08-13
MX9703957A (en) 1997-09-30
SK74697A3 (en) 1997-11-05
AR001332A1 (en) 1997-10-22
NO972526D0 (en) 1997-06-03
CA2204130A1 (en) 1996-06-20
EP0797583A1 (en) 1997-10-01
TR199501568A2 (en) 1996-07-21
FI971685A0 (en) 1997-04-18
PL320217A1 (en) 1997-09-15
BR9509997A (en) 1997-12-30
NO972526L (en) 1997-06-03
CZ179097A3 (en) 1997-10-15
AU4343796A (en) 1996-07-03
JPH10511935A (en) 1998-11-17
HUT77002A (en) 1998-03-02
CO4700289A1 (en) 1998-12-29

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Legal Events

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FG Grant, registration
FD Application declared void or lapsed