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PE20010745A1 - Diazepanes como inhibidores de la interaccion del antigeno lfa-1 y la molecula de adhesion intracelular (icam) - Google Patents

Diazepanes como inhibidores de la interaccion del antigeno lfa-1 y la molecula de adhesion intracelular (icam)

Info

Publication number
PE20010745A1
PE20010745A1 PE2000001087A PE0010872000A PE20010745A1 PE 20010745 A1 PE20010745 A1 PE 20010745A1 PE 2000001087 A PE2000001087 A PE 2000001087A PE 0010872000 A PE0010872000 A PE 0010872000A PE 20010745 A1 PE20010745 A1 PE 20010745A1
Authority
PE
Peru
Prior art keywords
alkyl
icam
naphthylmethyl
arylalkyl
alkylene
Prior art date
Application number
PE2000001087A
Other languages
English (en)
Inventor
Rainer Albert
Gabriele Weitz-Schmidt
Jorg Kallen
Ulrich Hommel
Sompong Wattanasin
Claus Ehrhardt
Josef Gottfried Meingassner
Didier Roche
Karld Welzenbach
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
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20010745A1 publication Critical patent/PE20010745A1/es

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
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    • 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Biophysics (AREA)

Abstract

SE REFIERE A DIAZEPAN DE FORMULA I, DONDE n ES 1-3; R1 ES H, ALQUILO C1-C4, ARILO, ARILALQUILO C1-C4; Y ES ALQUILENO C1-C4, CO-CH2-ALQUILENO C1-C4, CO-CH2-ALQUENILENO C2-C5, CONH; R2 ES UN RESIDUO AROMATICO, HETEROAROMATICO OPCIONALMENTE SUSTITUIDO CON CF3, HALOGENO, OH, ALCOXILO C1-C4, AMINO, FENILO, BENCILO, ALQUILO C1-C4; R3 ES UN O-AMINOACIDO; R4 ES BIFENILO, BENCILO, HIDROXIBENCILO, O-NAFTILMETILO, ß-NAFTILMETILO, 5,6,7,8-TETRAHIDRO-ß-NAFTILMETILO, INDOLILMETILO OPCIONALMENTE SUSTITUIDO SOBRE EL ANILLO POR CF3, HALOGENO, OH, ALCOXILO C1-C4, AMINO, ENTRE OTROS; X ES CN, NR5R6, OR8; R5 ES H, ALQUILO C1-C6, ARIL, ARILALQUILO C1-C4; R6 ES H, ALQUILO C1-C6; R7 ES H, ALQUILO C1-C4, ARILO, ARILALQUILO C1-C4. UN COMPUESTO PREFERIDO ES (R)-2-[(3S,5R)-5-METIL-2-OXO-3-FENIL-4-(QUINOLIN-6-IL-ACETIL)-[1,4]DIAZEPAN-1-IL]-3-(NAFTALEN-1-IL)PROPIONAMIDA. TAMBIEN SE REFIERE A UN PROCESO PARA LA PREPARACION; A UNA COMPOSICION QUE COMPRENDE ADEMAS UN FARMACO INMUNOSUPRESOR, INMUNOMODULADOR, ANTIINFLAMATORIO. EL COMPUESTO I ES UN INHIBIDOR DE LAS INTERACCIONES DEL ANTIGENO LFA-1 Y LA MOLECULA DE ADHESION INTRACELULAR ICAM-1, -ICAM-2, -ICAM-3, O INHIBEN LA INFLAMACION Y PUEDE SER UTIL PARA EL TRATAMIENTO DE LA ISQUEMIA, LESION POR REPERFUSION, INFARTO AL MIOCARDIO, EMBOLIA, ISQUEMIA DEL INTESTINO, DESORDENES INFLAMATORIOS AGUDOS
PE2000001087A 1999-10-13 2000-10-11 Diazepanes como inhibidores de la interaccion del antigeno lfa-1 y la molecula de adhesion intracelular (icam) PE20010745A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US41681599A 1999-10-13 1999-10-13

Publications (1)

Publication Number Publication Date
PE20010745A1 true PE20010745A1 (es) 2001-07-17

Family

ID=23651420

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001087A PE20010745A1 (es) 1999-10-13 2000-10-11 Diazepanes como inhibidores de la interaccion del antigeno lfa-1 y la molecula de adhesion intracelular (icam)

Country Status (12)

Country Link
EP (1) EP1220852B1 (es)
JP (1) JP3889623B2 (es)
AT (1) ATE316084T1 (es)
AU (1) AU7918500A (es)
CO (1) CO5251460A1 (es)
CY (1) CY1105020T1 (es)
DE (1) DE60025639T2 (es)
DK (1) DK1220852T3 (es)
EC (1) ECSP003707A (es)
ES (1) ES2257328T3 (es)
PE (1) PE20010745A1 (es)
WO (1) WO2001027102A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6867203B2 (en) 1998-12-29 2005-03-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
US6110922A (en) 1998-12-29 2000-08-29 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
US6521619B2 (en) 2000-06-29 2003-02-18 Icos Corporation Aryl phenylcyclopropyl sulfide derivatives and their use as cell adhesion inhibiting anti-inflammatory and immune suppressive agents
WO2002002539A1 (en) 2000-06-29 2002-01-10 Abbott Laboratories Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
AR030817A1 (es) 2000-10-02 2003-09-03 Novartis Ag Derivados de diazacicloalcanodiona
TWI311557B (en) 2003-01-23 2009-07-01 Novartis A Pharmaceutically active diazepanes
GB0301561D0 (en) * 2003-01-23 2003-02-26 Novartis Ag Organic compounds
PT1682537E (pt) 2003-11-05 2012-06-20 Sarcode Bioscience Inc Moduladores de adesão celular
US7943660B2 (en) 2005-04-15 2011-05-17 Dominion Pharmakine S.L. Inhibitors of the LFA-1/ICAM-1 interaction and uses thereof
GB0507918D0 (en) * 2005-04-19 2005-05-25 Novartis Ag Organic compounds
CA2960117C (en) 2005-05-17 2018-01-30 Sarcode Bioscience Inc. Lfa-1 antagonists for the treatment of eye disorders
US20090155176A1 (en) 2007-10-19 2009-06-18 Sarcode Corporation Compositions and methods for treatment of diabetic retinopathy
US8080562B2 (en) 2008-04-15 2011-12-20 Sarcode Bioscience Inc. Crystalline pharmaceutical and methods of preparation and use thereof
WO2011050175A1 (en) 2009-10-21 2011-04-28 Sarcode Corporation Crystalline pharmaceutical and methods of preparation and use thereof
GB201016864D0 (en) 2010-10-06 2010-11-17 Univ Aston Therapeutic methods
EP2877465A4 (en) 2012-07-25 2016-05-11 Sarcode Bioscience Inc LFA-1 HEMMER AND POLYMORPH THEREOF

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL92011A0 (en) * 1988-10-19 1990-07-12 Abbott Lab Heterocyclic peptide renin inhibitors
PL294870A1 (es) * 1991-06-21 1993-02-08 Hoechst Ag
AU1083499A (en) * 1997-10-21 1999-05-10 Pharmacia & Upjohn Company Thiadiazoles amides useful as antiinflammatory agents

Also Published As

Publication number Publication date
EP1220852A1 (en) 2002-07-10
ATE316084T1 (de) 2006-02-15
EP1220852B1 (en) 2006-01-18
DK1220852T3 (da) 2006-05-15
ES2257328T3 (es) 2006-08-01
WO2001027102A1 (en) 2001-04-19
AU7918500A (en) 2001-04-23
JP2003511447A (ja) 2003-03-25
DE60025639D1 (de) 2006-04-06
CY1105020T1 (el) 2010-03-03
DE60025639T2 (de) 2006-11-16
ECSP003707A (es) 2002-05-23
JP3889623B2 (ja) 2007-03-07
CO5251460A1 (es) 2003-02-28

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