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PE20010961A1 - 4-pirimidinil-n-acil-l-fenilalaninas utiles para el tratamiento de enfermedades inflamatorias cronicas - Google Patents

4-pirimidinil-n-acil-l-fenilalaninas utiles para el tratamiento de enfermedades inflamatorias cronicas

Info

Publication number
PE20010961A1
PE20010961A1 PE2000001293A PE0012932000A PE20010961A1 PE 20010961 A1 PE20010961 A1 PE 20010961A1 PE 2000001293 A PE2000001293 A PE 2000001293A PE 0012932000 A PE0012932000 A PE 0012932000A PE 20010961 A1 PE20010961 A1 PE 20010961A1
Authority
PE
Peru
Prior art keywords
alkyl
aryl
pyrimidinyl
acil
useful
Prior art date
Application number
PE2000001293A
Other languages
English (en)
Inventor
Tilley Jefferson Wright
Achyutharao Sidduri
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20010961A1 publication Critical patent/PE20010961A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A 4-PIRIMIDINIL-N-ACIL-L-FENILALANINA DE FORMULA I; DONDE R1 ES Y-1, UN ANILLO HETEROAROMATICO DE 5-6 MIEMBROS; Y-3; R22, R23 SON H, ALQUILO, ALCOXI, ARILALQUILO, ENTRE OTROS; R24 ES H, ALQUILO, ARILO, NITRO, ENTRE OTROS; R25 ES ALQUILO, ALQUENILO, R26-(CH2)e-; R26 ES ARILO, HETEROARILO, AZIDO, NR28R29, ENTRE OTROS; R28 ES H, ALQUILO; R29 ES H, ALQUILO, ALCOXI-CARBONILO, ENTRE OTROS; O R28 Y R29 JUNTO A N FORMAN UN HETEROCICLO DE 4-6 MIEMBROS; Q ES (CH2)fO-, (CH2)fS, (CH2)fN(R27), ENTRE OTROS; R27 ES H, ALQUILO, ARILO, ALCANOILO, ENTRE OTROS; R40 ES H, ALQUILO, ARILO, ENTRE OTROS; e ES 0-4; f ES 0-3; R2 ES H, ALQUILO, ARILALQUILO, ARILO, R3 ES H, ALQUILO, ARILALQUILO, ARILO, ENTRE OTROS; R4 ES H, HALOGENO, ALQUILO, ENTRE OTROS; R5 ES H, ALQUILO, CLORO, CARBOXI; R6 ES H, ALQUILO, P-3, P-4; R32, R33, R34 SON H, ALQUILO; h, g, j SON DE 0-2; h+g ES 1-3; Q' ES O, S, (CH2)j, NR35; R35 ES H, ALQUILO, ALCANOILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS N-[(2,6-DICLOROFENIL)CARBONIL]-4-(1,3,6-TRIMETIL-2,4-DIOXO-5-PIRIMIDINIL)-L-FENILALANINA, N-[(2-BROMO-6-METILFENIL)CARBONIL]-4-(1,3,6-TRIMETIL-2,4-DIOXO-5-PIRIMIDINIL)-L-FENILALANINA, ENTRE OTROS. EL COMPUESTO I INHIBE LA UNION DE MOLECULA-1 DE ADHESION A CELULAS VASCULARES VCAM-1, ANTIGENO VLA-4, CELULAS DE EXPRESION DE VLA-4 POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DE ARTRITIS REUMATOIDE, ESCLEROSIS MULTIPLE, ENFERMEDADES INFLAMATORIAS INTESTINALES, ASMA
PE2000001293A 1999-12-06 2000-12-05 4-pirimidinil-n-acil-l-fenilalaninas utiles para el tratamiento de enfermedades inflamatorias cronicas PE20010961A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16908999P 1999-12-06 1999-12-06

Publications (1)

Publication Number Publication Date
PE20010961A1 true PE20010961A1 (es) 2001-09-26

Family

ID=22614222

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001293A PE20010961A1 (es) 1999-12-06 2000-12-05 4-pirimidinil-n-acil-l-fenilalaninas utiles para el tratamiento de enfermedades inflamatorias cronicas

Country Status (35)

Country Link
EP (1) EP1237878B1 (es)
JP (1) JP3824935B2 (es)
KR (1) KR100522344B1 (es)
CN (1) CN1218943C (es)
AR (1) AR034401A1 (es)
AT (1) ATE357433T1 (es)
AU (1) AU783348B2 (es)
BR (1) BR0016195A (es)
CA (1) CA2392570C (es)
CO (1) CO5080772A1 (es)
CY (1) CY1106626T1 (es)
CZ (1) CZ303435B6 (es)
DE (1) DE60034061T2 (es)
DK (1) DK1237878T3 (es)
EG (1) EG24361A (es)
ES (1) ES2282162T3 (es)
HK (1) HK1054384B (es)
HR (1) HRP20020468B1 (es)
HU (1) HU229105B1 (es)
IL (2) IL149617A0 (es)
JO (1) JO2283B1 (es)
MA (1) MA26850A1 (es)
MX (1) MXPA02005564A (es)
MY (1) MY126972A (es)
NO (1) NO322866B1 (es)
NZ (1) NZ518828A (es)
PE (1) PE20010961A1 (es)
PL (1) PL207160B1 (es)
PT (1) PT1237878E (es)
RS (1) RS50371B (es)
RU (1) RU2266901C2 (es)
SI (1) SI1237878T1 (es)
TW (1) TWI256387B (es)
WO (1) WO2001042225A2 (es)
ZA (1) ZA200203533B (es)

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AR033765A1 (es) * 2001-05-22 2004-01-07 Syngenta Participations Ag Procedimiento para la preparacion de derivados 3-alquil-3h-isobenzofuran-1-ona 7-sustituidos.
WO2003053926A1 (en) 2001-12-13 2003-07-03 Ajinomoto Co.,Inc. Novel phenylalanine derivative
EP1700850B1 (en) 2003-12-22 2015-07-15 Ajinomoto Co., Inc. Phenylalanine derivative
US7618981B2 (en) * 2004-05-06 2009-11-17 Cytokinetics, Inc. Imidazopyridinyl-benzamide anti-cancer agents
WO2006023396A2 (en) * 2004-08-16 2006-03-02 Merck & Co., Inc. Vla-4 antagonists
JP4784224B2 (ja) 2004-09-24 2011-10-05 味の素株式会社 糖鎖転移方法および糖鎖転移酵素
US20090137601A1 (en) * 2005-11-23 2009-05-28 Astrazeneca Ab L-Phenylalanine Derivatives
AR059224A1 (es) * 2006-01-31 2008-03-19 Jerini Ag Compuestos para la inhibicion de integrinas y uso de estas
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JP6159740B2 (ja) * 2012-01-27 2017-07-05 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Vla−4を発現する細胞への標的化送達のためのインテグリンアンタゴニスト結合体
US9447035B2 (en) * 2012-01-27 2016-09-20 Hoffmann-La Roche Inc. Integrin antagonist conjugates for targeted delivery to cells expressing VLA-4
WO2015048819A1 (en) 2013-09-30 2015-04-02 The Regents Of The University Of California Anti-alphavbeta1 integrin compounds and methods
PT3064491T (pt) * 2013-10-29 2020-02-20 Ea Pharma Co Ltd Derivado de sulfonamida e sua utilização medicinal
CA2981371A1 (en) 2015-03-10 2016-09-15 The Regents Of The University Of California Anti-alphavbeta1 integrin inhibitors and methods of use
CA3115820A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. Compounds for inhibition of .alpha.4.beta.7 integrin
ES3003232T3 (en) 2018-10-30 2025-03-10 Gilead Sciences Inc Compounds for inhibition of alpha4beta7 integrin
CN112969687B (zh) 2018-10-30 2024-08-23 吉利德科学公司 作为α4β7整合素抑制剂的喹啉衍生物
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HK1045495A1 (zh) * 1999-01-22 2002-11-29 依兰制药公司 抑制vla-4介导的白细胞粘着的多环化合物

Also Published As

Publication number Publication date
CA2392570A1 (en) 2001-06-14
HRP20020468B1 (en) 2009-02-28
EG24361A (en) 2009-03-04
JO2283B1 (en) 2005-09-12
DK1237878T3 (da) 2007-07-30
AU2669601A (en) 2001-06-18
CA2392570C (en) 2010-05-11
DE60034061T2 (de) 2007-12-13
HRP20020468A2 (en) 2004-04-30
NO20022633D0 (no) 2002-06-04
HK1054384B (zh) 2005-12-09
HU229105B1 (en) 2013-07-29
AR034401A1 (es) 2004-02-25
PL207160B1 (pl) 2010-11-30
SI1237878T1 (sl) 2007-08-31
CN1218943C (zh) 2005-09-14
AU783348B2 (en) 2005-10-20
ES2282162T3 (es) 2007-10-16
JP3824935B2 (ja) 2006-09-20
HUP0204081A2 (en) 2003-05-28
CZ303435B6 (cs) 2012-09-12
NO322866B1 (no) 2006-12-18
IL149617A0 (en) 2002-11-10
EP1237878A2 (en) 2002-09-11
CY1106626T1 (el) 2012-01-25
DE60034061D1 (de) 2007-05-03
PT1237878E (pt) 2007-06-18
YU40402A (sh) 2005-03-15
WO2001042225A2 (en) 2001-06-14
NO20022633L (no) 2002-06-04
CO5080772A1 (es) 2001-09-25
NZ518828A (en) 2004-03-26
CN1407972A (zh) 2003-04-02
MY126972A (en) 2006-11-30
RU2266901C2 (ru) 2005-12-27
KR20020063906A (ko) 2002-08-05
EP1237878B1 (en) 2007-03-21
ATE357433T1 (de) 2007-04-15
RU2002117422A (ru) 2004-03-10
HUP0204081A3 (en) 2003-07-28
TWI256387B (en) 2006-06-11
MA26850A1 (fr) 2004-12-20
JP2003516396A (ja) 2003-05-13
MXPA02005564A (es) 2002-09-02
ZA200203533B (en) 2003-08-04
WO2001042225A3 (en) 2002-02-21
RS50371B (sr) 2009-11-10
CZ20022351A3 (cs) 2003-04-16
KR100522344B1 (ko) 2005-10-20
WO2001042225A8 (en) 2002-06-06
HK1054384A1 (en) 2003-11-28
IL149617A (en) 2007-10-31
BR0016195A (pt) 2002-08-13
PL357601A1 (en) 2004-07-26

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