BR0016195A - 4-pirimidinil-n-acil-l-fenilalaninas - Google Patents

4-pirimidinil-n-acil-l-fenilalaninas

Info

Publication number
BR0016195A
BR0016195A BR0016195-0A BR0016195A BR0016195A BR 0016195 A BR0016195 A BR 0016195A BR 0016195 A BR0016195 A BR 0016195A BR 0016195 A BR0016195 A BR 0016195A
Authority
BR
Brazil
Prior art keywords
pyrimidinyl
acyl
phenylalanines
vcam
binding
Prior art date
Application number
BR0016195-0A
Other languages
English (en)
Inventor
Achyutharao Sidduri
Jefferson Wright Tilley
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 BR0016195A publication Critical patent/BR0016195A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/28—Drugs 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
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two 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
    • C07D239/553—Two 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (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)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

"4-PIRIMIDINIL-N-ACIL-L-FENILALANINAS". A presente invenção refere-se a compostos de fórmula (1), em que R^ 1^ a R^ 6^ São como definidos no relatório descritivo e que são inibidores de ligação entre VCAM-1 e células expressando VLA-4, e por conseguinte são úteis para o tratamento de doenças cujos sintomas e/ou danos estão relacionados com a ligação de VCAM-1 a células expressando VLA-4.
BR0016195-0A 1999-12-06 2000-11-28 4-pirimidinil-n-acil-l-fenilalaninas BR0016195A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16908999P 1999-12-06 1999-12-06
PCT/EP2000/011884 WO2001042225A2 (en) 1999-12-06 2000-11-28 4-pyrimidinyl-n-acyl-l-phenylalanines

Publications (1)

Publication Number Publication Date
BR0016195A true BR0016195A (pt) 2002-08-13

Family

ID=22614222

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0016195-0A BR0016195A (pt) 1999-12-06 2000-11-28 4-pirimidinil-n-acil-l-fenilalaninas

Country Status (35)

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

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6960597B2 (en) 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
ATE497385T1 (de) 2000-08-18 2011-02-15 Ajinomoto Kk Neue phenylalanin-derivate
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
CN101006097B (zh) * 2004-08-16 2012-07-11 默沙东公司 Vla-4拮抗剂
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
EP2091916A2 (en) * 2005-11-23 2009-08-26 AstraZeneca AB L-phenylalanine derivatives and their use as integrin antagonists
AR059224A1 (es) * 2006-01-31 2008-03-19 Jerini Ag Compuestos para la inhibicion de integrinas y uso de estas
JP2009526032A (ja) * 2006-02-09 2009-07-16 アストラゼネカ アクチボラグ 化合物
ATE556061T1 (de) * 2006-06-19 2012-05-15 Toray Industries Therapeutisches oder prophylaktisches mittel gegen multiple sklerose
DK2203431T3 (da) 2007-09-17 2011-11-21 Abbott Lab Antiinfektiøse pyrimidiner og anvendelser heraf
TWI534137B (zh) * 2007-09-17 2016-05-21 艾伯維巴哈馬有限公司 抗感染劑及其用途
WO2009039135A1 (en) 2007-09-17 2009-03-26 Abbott Laboratories N-phenyl-dioxo-hydropyrimidines useful as hepatitis c virus (hcv) inhibitors
TWI448470B (zh) * 2008-12-22 2014-08-11 Icl Ip America Inc 基於水互溶性溶劑的方法
US9216952B2 (en) 2010-03-23 2015-12-22 Abbvie Inc. Process for preparing antiviral compound
US8975443B2 (en) 2010-07-16 2015-03-10 Abbvie Inc. Phosphine ligands for catalytic reactions
WO2012009699A2 (en) 2010-07-16 2012-01-19 Abbott Laboratories Process for preparing antiviral compounds
US9255074B2 (en) 2010-07-16 2016-02-09 Abbvie Inc. Process for preparing antiviral compounds
BR112013001138A2 (pt) 2010-07-16 2016-07-05 Abbvie Inc ligantes de fosfina para reações catalíticas
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
US9447035B2 (en) * 2012-01-27 2016-09-20 Hoffmann-La Roche Inc. Integrin antagonist conjugates for targeted delivery to cells expressing VLA-4
CN104023751B (zh) * 2012-01-27 2016-11-09 弗·哈夫曼-拉罗切有限公司 靶向递送至表达vla-4的细胞的整联蛋白拮抗剂结合物
WO2015048819A1 (en) 2013-09-30 2015-04-02 The Regents Of The University Of California Anti-alphavbeta1 integrin compounds and methods
ES2778200T3 (es) 2013-10-29 2020-08-10 Ea Pharma Co Ltd Derivado de sulfonamida y su uso medicinal
CA2981371A1 (en) 2015-03-10 2016-09-15 The Regents Of The University Of California Anti-alphavbeta1 integrin inhibitors and methods of use
AU2019373242B2 (en) 2018-10-30 2023-07-13 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
KR102630416B1 (ko) 2018-10-30 2024-02-01 길리애드 사이언시즈, 인코포레이티드 알파4베타7 인테그린 억제제로서의 퀴놀린 유도체
ES3013256T3 (en) 2018-10-30 2025-04-11 Gilead Sciences Inc Imidazo[1,2-a]pyridine derivatives as alpha4beta7 integrin inhibitors for the treatment of inflammatory diseases
US11179383B2 (en) 2018-10-30 2021-11-23 Gilead Sciences, Inc. Compounds for inhibition of α4β7 integrin
CN114222730B (zh) 2019-08-14 2024-09-10 吉利德科学公司 用于抑制α4β7整合素的化合物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH516578A (de) * 1967-11-02 1971-12-15 Bayer Ag Verfahren zur Herstellung von heterocyclische Acylaminogruppen enthaltenden Arylsulfonylharnstoffen mit blutdrucksenkender Wirkung
EP1001764A4 (en) * 1997-05-29 2005-08-24 Merck & Co Inc HETEROCYCLIC AMIDE COMPOUNDS AS INHIBITORS OF CELL ADHESION
DE69833654T2 (de) * 1997-05-29 2006-12-14 Merck & Co., Inc. (A New Jersey Corp.) Biarylalkansäuren in der verwendung als zelladhäsionsinhibitoren
ATE267801T1 (de) * 1997-08-22 2004-06-15 Hoffmann La Roche N-alkanoylphenylalaninderivate
DE69821950T2 (de) * 1997-08-22 2004-12-16 F. Hoffmann-La Roche Ag N-aroylphenylalaninderivate
CA2357781A1 (en) * 1999-01-22 2000-07-27 Elan Pharmaceuticals, Inc. Multicyclic compounds which inhibit leukocyte adhesion mediated by vla-4

Also Published As

Publication number Publication date
MXPA02005564A (es) 2002-09-02
AU783348B2 (en) 2005-10-20
CA2392570C (en) 2010-05-11
SI1237878T1 (sl) 2007-08-31
NZ518828A (en) 2004-03-26
PL207160B1 (pl) 2010-11-30
HUP0204081A3 (en) 2003-07-28
KR20020063906A (ko) 2002-08-05
CZ303435B6 (cs) 2012-09-12
PT1237878E (pt) 2007-06-18
NO20022633L (no) 2002-06-04
CN1407972A (zh) 2003-04-02
MA26850A1 (fr) 2004-12-20
CN1218943C (zh) 2005-09-14
RU2266901C2 (ru) 2005-12-27
WO2001042225A8 (en) 2002-06-06
NO20022633D0 (no) 2002-06-04
JP2003516396A (ja) 2003-05-13
AU2669601A (en) 2001-06-18
CY1106626T1 (el) 2012-01-25
KR100522344B1 (ko) 2005-10-20
ATE357433T1 (de) 2007-04-15
PE20010961A1 (es) 2001-09-26
MY126972A (en) 2006-11-30
CZ20022351A3 (cs) 2003-04-16
PL357601A1 (en) 2004-07-26
WO2001042225A3 (en) 2002-02-21
CO5080772A1 (es) 2001-09-25
TWI256387B (en) 2006-06-11
CA2392570A1 (en) 2001-06-14
EP1237878B1 (en) 2007-03-21
ES2282162T3 (es) 2007-10-16
DE60034061T2 (de) 2007-12-13
ZA200203533B (en) 2003-08-04
JO2283B1 (en) 2005-09-12
IL149617A (en) 2007-10-31
HU229105B1 (en) 2013-07-29
AR034401A1 (es) 2004-02-25
RU2002117422A (ru) 2004-03-10
EP1237878A2 (en) 2002-09-11
YU40402A (sh) 2005-03-15
NO322866B1 (no) 2006-12-18
DE60034061D1 (de) 2007-05-03
DK1237878T3 (da) 2007-07-30
HK1054384B (zh) 2005-12-09
WO2001042225A2 (en) 2001-06-14
EG24361A (en) 2009-03-04
HRP20020468A2 (en) 2004-04-30
HUP0204081A2 (en) 2003-05-28
HRP20020468B1 (en) 2009-02-28
HK1054384A1 (en) 2003-11-28
IL149617A0 (en) 2002-11-10
RS50371B (sr) 2009-11-10
JP3824935B2 (ja) 2006-09-20

Similar Documents

Publication Publication Date Title
TWI256387B (en) 4-pyrimidinyl-n-acyl-l-phenylalanines
BR9811988A (pt) Derivados de n-alcanoilfenilalanina
DE69824183T2 (de) N-alkanoylphenylalaninderivate
BR0016172A (pt) 4-piridinil-n-acil-l-fenilalaninas
BR0309556A (pt) Inibidores de metaloproteinase pirimidina-2,4,6-triona
BR0314379A (pt) Quinazolinonas espirocondensadas e a sua utilização como inibidores de fosfodiesterase
SE0301888D0 (sv) New use VII
BR0007527A (pt) Fenilfenantridinas com atividade inibitória depde-iv
BRPI0409624A (pt) 2-hidróxi-3-diaminoalcanos de benzamida
EA200802054A1 (ru) Ингибиторы фермента
BR9908480A (pt) Compostos heterocìclicos como inibidores de enzimas rotamase
BRPI0415203A (pt) pentanóis reestruturados, um processo para sua produção e seu uso como agentes antiinflamatórios
BRPI0407913A (pt) antagonistas receptores de ccr-3
BRPI0607019A2 (pt) compostos que inibem a atividade de beta -secretase e métodos de uso dos mesmos
BRPI0512784A (pt) tetrahidroquinolinas
BR0112543A (pt) Derivados hidrazìdicos do ácido pirrolidino-2-carboxìlico para uso como inibidores de metaloproteases
DK1244614T3 (da) Tryptase-inhibitorer
BRPI0417140A (pt) derivados quinolina ácidos e seu uso na prevenção e/ou tratamento de patologias relacionadas com hiperglicemia
BRPI0607560A2 (pt) derivados de tienopiridina e o uso dos mesmos como moduladores de hsp90
ATE348803T1 (de) Tryptase-inhibitoren
ECSP003806A (es) 4-piridinil-n-acil-l-fenilalaninas
BRPI0416570A (pt) processo para preparação de 4-pentafluorsulfanil-benzoilguanidinas
ECSP003805A (es) 4-piridinil-n-acil-l-fenilalaninas
UY26471A1 (es) 4- pirimidinil - n - acil - l - fenilalaninas
AR015936A1 (es) Derivados de n-alcanoilfenilalanina, medicamento que los contiene, procedimiento para la produccion de dicho medicamento y su empleo en terapia

Legal Events

Date Code Title Description
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFIRO O PEDIDO DE ACORDO COM O(S) ARTIGO(S) 8O,13, 24, 25 DA LPI

B12B Appeal against refusal [chapter 12.2 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B11D Dismissal acc. art. 38, par 2 of ipl - failure to pay fee after grant in time