AR019415A1 - DERIVATIVES OF BIFENYLL, A PROCEDURE FOR THEIR PREPARATION, ITS EMPLOYMENT IN THE PREPARATION OF MEDICINES, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS - Google Patents

DERIVATIVES OF BIFENYLL, A PROCEDURE FOR THEIR PREPARATION, ITS EMPLOYMENT IN THE PREPARATION OF MEDICINES, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS

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Publication number
AR019415A1
AR019415A1 ARP990103510A ARP990103510A AR019415A1 AR 019415 A1 AR019415 A1 AR 019415A1 AR P990103510 A ARP990103510 A AR P990103510A AR P990103510 A ARP990103510 A AR P990103510A AR 019415 A1 AR019415 A1 AR 019415A1
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AR
Argentina
Prior art keywords
formula
compound
procedure
preparation
piperidinyl
Prior art date
Application number
ARP990103510A
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Spanish (es)
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Merck Patent Gmbh
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.)
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Publication date
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Publication of AR019415A1 publication Critical patent/AR019415A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids

Abstract

Derivados de bifenilo de formula (1) en donde R representa -C(=NH)-NH2, -C(=NH)-NHA3, -C(=NH)-NHAc, -C(=NH) -NHSO2CH3, R2, -CO-NH-Z-R3 o -CO-R1, Xrepresenta -CONH-, SO2NH-, -NHCO- o -NHSO2, Y representa CH o N, A1 representa H, alquilo de 1 a 6 átomos de C en el cual 1 a 7 átomos de H pueden estarreeemplazados por F, SO2CH3, o SO2CF3, A2 representa H o alquilo de 1 a 6 átomos de C, A3, A5 representan independientemente alquilo C1-6, A6, A7representan independientemente H o (CH2)pCH3, Q representa H o OA1, R representa 4-A5-piperazin-1-ilo, 4-A5-homopiperazinilo, 1-pirrolidinilo monosustituidocon R4 o Z-R4, 1 piperidinilo monosustituido con R4 o Z-R4, N-A5-pirrolidinil-amino, N-A5-piperidinil-amino, N-A5-pirrolidinil-Z-amino, N-A5-piperidinil-Z-amino, -N(A6) (ZR3) o NA6A7, R2 representa 5-metil-1, 3, 4 -oxadiazol-2-ilo o 5- metil-1,2,4-oxadiazol-3-ilo, R3, R4 representan independientemente NHA5,N(A5)2, 4-morfolinilo, 1-pirrolidinilo o 1-piperidinilo, Z representa alquileno de 1 a 6 átomos de C, n es 0 o 1, p es 0, 1 o 2, con la condicion de que cuandoY representa N, X=CONH- y n=1, entonces R no es R2 o R no es -CONA6A7, incluyendo los racematos, los enantiomeros, las sales aceptables desde el punto de vistafisiologico y los solvatos de estos compuestos. Un procedimiento para preparar los compuestos de formula I, sus sales y sus solvatos, en el cual a) se hacereaccionar un compuesto de formula II en donde L representa Cl, Br, I o un grupo OH transformado funcionalmente en ungrupo reactivo, y R y A3 tienen lossignificados indicados más arriba, con un derivado del ácido boronico de formula III en donde X, Y, A1, A2 Q y n tienen los significados indicados más arriba ob) se hace reaccionar un compuesto de formula IV en donde R y A3 y L tienen los significados indicados, X representa CO o SO2, con un compuesto de formula Ven donde Y, A1, A2 y n tienen los significados indicados o c) para preparar un compuesto de formula I en donde R representa -CO-NH--Z-R3 o -CO-R1 se hacereaccionar un compuesto de formula VI en donde L representa Cl, Br, I o un grupo OH libre o transformado funcionalmente en un grupo reactivo, y X, Y, A1,A2, A3Biphenyl derivatives of formula (1) wherein R represents -C (= NH) -NH2, -C (= NH) -NHA3, -C (= NH) -NHAc, -C (= NH) -NHSO2CH3, R2, -CO-NH-Z-R3 or -CO-R1, X represents -CONH-, SO2NH-, -NHCO- or -NHSO2, Y represents CH or N, A1 represents H, alkyl of 1 to 6 C atoms in which 1 to 7 atoms of H may be replaced by F, SO2CH3, or SO2CF3, A2 represents H or alkyl of 1 to 6 atoms of C, A3, A5 independently represent C1-6 alkyl, A6, A7 independently represent H or (CH2) pCH3, Q represents H or OA1, R represents 4-A5-piperazin-1-yl, 4-A5-homopiperazinyl, 1-pyrrolidinyl monosubstituted with R4 or Z-R4, 1 piperidinyl monosubstituted with R4 or Z-R4, N-A5-pyrrolidinyl- amino, N-A5-piperidinyl-amino, N-A5-pyrrolidinyl-Z-amino, N-A5-piperidinyl-Z-amino, -N (A6) (ZR3) or NA6A7, R2 represents 5-methyl-1, 3 , 4-oxadiazol-2-yl or 5- methyl-1,2,4-oxadiazol-3-yl, R3, R4 independently represent NHA5, N (A5) 2,4-morpholinyl, 1-pyrrolidinyl or 1-piperidinyl, Z represents alkylene from 1 to 6 volumes of C, n is 0 or 1, p is 0, 1 or 2, with the proviso that when Y represents N, X = CONH- and n = 1, then R is not R2 or R is not -CONA6A7, including racemates , enantiomers, physiologically acceptable salts and solvates of these compounds. A process for preparing the compounds of formula I, their salts and their solvates, in which a) a compound of formula II is reacted wherein L represents Cl, Br, I or an OH group functionally transformed into a reactive group, and R and A3 have the meanings indicated above, with a boronic acid derivative of formula III where X, Y, A1, A2 Q and n have the meanings indicated above or b) a compound of formula IV is reacted where R and A3 and L they have the indicated meanings, X represents CO or SO2, with a compound of formula Ven where Y, A1, A2 and n have the meanings indicated oc) to prepare a compound of formula I wherein R represents -CO-NH-Z-R3 or -CO-R1 is reacted a compound of formula VI wherein L represents Cl, Br, I or a free or functionally transformed OH group in a reactive group, and X, Y, A1, A2, A3

ARP990103510A 1998-07-20 1999-07-16 DERIVATIVES OF BIFENYLL, A PROCEDURE FOR THEIR PREPARATION, ITS EMPLOYMENT IN THE PREPARATION OF MEDICINES, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS AR019415A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP98113488 1998-07-20

Publications (1)

Publication Number Publication Date
AR019415A1 true AR019415A1 (en) 2002-02-20

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ARP990103510A AR019415A1 (en) 1998-07-20 1999-07-16 DERIVATIVES OF BIFENYLL, A PROCEDURE FOR THEIR PREPARATION, ITS EMPLOYMENT IN THE PREPARATION OF MEDICINES, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS

Country Status (15)

Country Link
EP (1) EP1098892A1 (en)
JP (1) JP2002521377A (en)
KR (1) KR20010070997A (en)
CN (1) CN1309654A (en)
AR (1) AR019415A1 (en)
AU (1) AU5033899A (en)
BR (1) BR9912299A (en)
CA (1) CA2338209A1 (en)
HU (1) HUP0102622A3 (en)
ID (1) ID27846A (en)
NO (1) NO20010333D0 (en)
PL (1) PL345283A1 (en)
SK (1) SK492001A3 (en)
WO (1) WO2000005225A1 (en)
ZA (1) ZA200101379B (en)

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US7718650B2 (en) 2001-05-11 2010-05-18 Biovitrum Ab Aryl sulfonamide compounds for treating obesity
CN1329382C (en) * 2001-05-11 2007-08-01 比奥维特罗姆股份公司 Novel arylsusfonamide compounds for treatment of obesity, type II diabetes and CNS-disorders
EP1429765A2 (en) 2001-09-14 2004-06-23 Methylgene, Inc. Inhibitors of histone deacetylase
SE0103644D0 (en) * 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic isoquinoline compounds
BRPI0513713A (en) 2004-07-28 2008-05-13 Glaxo Group Ltd piperazine derivatives useful for the treatment of gastrointestinal disorders
CN101039904B (en) * 2004-10-14 2014-09-24 Abbvie德国有限责任两合公司 Heterocyclic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor
WO2007077457A2 (en) * 2006-01-06 2007-07-12 The Royal Veterinary College Treatment of equine laminitis with 5-ht1b/ 1d antagonists
AR060213A1 (en) 2006-03-31 2008-06-04 Glaxo Group Ltd PIPERAZINIL COMPOUND - PIRIDINIL-BENCENSULFONAMIDE, ITS USE TO MANUFACTURE A MEDICINAL PROCESS FOR THE PREPARATION OF THE SAME PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND PROCESS TO PREPARE IT
US8497273B2 (en) 2006-04-19 2013-07-30 Abbott Gmbh & Co. Kg Heterocyclic compounds suitable for treating disorders that respond to modulation of the serotonin 5HT6 receptor
NZ572761A (en) 2006-04-19 2011-09-30 Abbott Gmbh & Co Kg Heterocyclic arylsulphones suitable for treating disorders that respond to modulation of the serotonin 5ht6 receptor
CN101432261A (en) 2006-05-19 2009-05-13 惠氏公司 N-benzoyl-and N-benzylpyrrolidin-3-ylamines as histamine-3 antagonists
NZ579766A (en) 2007-03-23 2012-03-30 Abbott Gmbh & Co Kg Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor
NZ581364A (en) 2007-06-05 2011-10-28 Nsab Af Neurosearch Sweden Ab Disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission
WO2008148851A1 (en) 2007-06-08 2008-12-11 Janssen Pharmaceutica N.V. Piperidine/piperazine derivatives
CA2687754C (en) 2007-06-08 2015-12-08 Janssen Pharmaceutica N.V. Piperidine, piperazine derivatives for use as dgat inhibitors
AU2008258549B2 (en) 2007-06-08 2013-11-14 Janssen Pharmaceutica N.V. Piperidine/piperazine derivatives
JO2972B1 (en) 2007-06-08 2016-03-15 جانسين فارماسوتيكا ان. في Piperidine/Piperazine derivatives
WO2009147170A2 (en) 2008-06-05 2009-12-10 Janssen Pharmaceutica Nv Drug combinations comprising a dgat inhibitor and a ppar-agonist

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GB9507203D0 (en) * 1995-04-07 1995-05-31 Smithkline Beecham Plc Novel compounds

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EP1098892A1 (en) 2001-05-16
ID27846A (en) 2001-04-26
NO20010333L (en) 2001-01-19
HUP0102622A3 (en) 2002-12-28
NO20010333D0 (en) 2001-01-19
WO2000005225A1 (en) 2000-02-03
CA2338209A1 (en) 2000-02-03
HUP0102622A2 (en) 2001-12-28
ZA200101379B (en) 2002-05-20
BR9912299A (en) 2001-11-20
AU5033899A (en) 2000-02-14
CN1309654A (en) 2001-08-22
PL345283A1 (en) 2001-12-03
SK492001A3 (en) 2001-08-06
JP2002521377A (en) 2002-07-16
KR20010070997A (en) 2001-07-28

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