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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (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
CA2420040C (en) * 2000-08-18 2009-02-03 Ajinomoto Co., Inc. New phenylalanine derivatives
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
US7345049B2 (en) 2003-12-22 2008-03-18 Ajinomoto Co., Inc. Phenylalanine derivatives
US7618981B2 (en) * 2004-05-06 2009-11-17 Cytokinetics, Inc. Imidazopyridinyl-benzamide anti-cancer agents
AU2005277634B2 (en) * 2004-08-16 2011-02-17 Merck Sharp & Dohme Corp. 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
JP2009516729A (ja) * 2005-11-23 2009-04-23 アストラゼネカ アクチボラグ Ｌ−フェニルアラニン誘導体
AR059224A1 (es) * 2006-01-31 2008-03-19 Jerini Ag Compuestos para la inhibicion de integrinas y uso de estas
CN101379028A (zh) * 2006-02-09 2009-03-04 阿斯利康(瑞典)有限公司 化学化合物
EP2039687B1 (en) 2006-06-19 2012-05-02 Toray Industries, Inc. Therapeutic or prophylactic agent for multiple sclerosis
PA8796201A1 (es) 2007-09-17 2009-04-23 Abbott Lab Agentes anti-infecciosos y su uso
PL2639226T3 (pl) 2007-09-17 2017-02-28 Abbvie Bahamas Ltd. Pirymidyny o działaniu przeciw zakaźnym oraz ich zastosowania
CN101918369B (zh) 2007-09-17 2016-02-24 艾伯维巴哈马有限公司 治疗丙型肝炎的尿嘧啶或胸腺嘧啶衍生物
CN102264747B (zh) * 2008-12-22 2014-09-24 Icl-Ip美国公司 基于水混溶性溶剂的二磷酸酯纯化用方法
US9216952B2 (en) 2010-03-23 2015-12-22 Abbvie Inc. Process for preparing antiviral compound
US9255074B2 (en) 2010-07-16 2016-02-09 Abbvie Inc. Process for preparing antiviral compounds
US8975443B2 (en) 2010-07-16 2015-03-10 Abbvie Inc. Phosphine ligands for catalytic reactions
CA2805748A1 (en) 2010-07-16 2012-01-19 Shashank Shekhar Process for preparing n-(6-(3-tert-butyl-5-(2,4-dioxo-3,4-dihydropyrimidin-1-(2h)-yl)-2-methoxyphenyl)naphthalen-2-yl)methanesulfonamide
SG187103A1 (en) 2010-07-16 2013-02-28 Abbvie Inc Phosphine ligands for catalytic reactions
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
EP2806898B1 (en) * 2012-01-27 2018-07-18 F.Hoffmann-La Roche Ag Integrin antagonist conjugates for targeted delivery to cells expressing vla-4
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
CN109053723B (zh) * 2013-10-29 2021-09-03 Ea制药株式会社 磺酰胺衍生物及其药物用途
WO2016145258A1 (en) 2015-03-10 2016-09-15 The Regents Of The University Of California Anti-alphavbeta1 integrin inhibitors and methods of use
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
JP7189368B2 (ja) 2018-10-30 2022-12-13 ギリアード サイエンシーズ， インコーポレイテッド アルファ４ベータ７インテグリンの阻害のための化合物
EP3873605B1 (en) 2018-10-30 2024-10-23 Gilead Sciences, Inc. Compounds for inhibition of alpha4beta7 integrin
FI3873884T3 (fi) 2018-10-30 2025-02-24 Gilead Sciences Inc 3-(kinolin-8-yyli)-1,4-dihydropyrido[3,4-d]pyrimidiini-2,4-dionijohdannaisia alfa-4-beta-7-integriinin estäjinä tulehdussairauksien hoidossa
WO2021030438A1 (en) 2019-08-14 2021-02-18 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin

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
JP2001517245A (ja) * 1997-05-29 2001-10-02 メルク エンド カンパニー インコーポレーテッド 細胞接着阻害薬としてのビアリールアルカン酸類
CN1276785A (zh) * 1997-08-22 2000-12-13 霍夫曼-拉罗奇有限公司 N－烷酰基苯丙氨酸衍生物
EP1005445B1 (en) * 1997-08-22 2004-05-26 F. Hoffmann-La Roche Ag N-alkanoylphenylalanine derivatives
US6465513B1 (en) * 1999-01-22 2002-10-15 Elan Pharmaceuticals, Inc. Multicyclic compounds which inhibit leukocyte adhesion mediated by VLA-4

Also Published As

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

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Legal Events

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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