CO5251460A1 - Diazepanes, proceso para su preparacion y composicion farmaceutica que los contiene - Google Patents

Diazepanes, proceso para su preparacion y composicion farmaceutica que los contiene

Info

Publication number
CO5251460A1
CO5251460A1 CO00077443A CO00077443A CO5251460A1 CO 5251460 A1 CO5251460 A1 CO 5251460A1 CO 00077443 A CO00077443 A CO 00077443A CO 00077443 A CO00077443 A CO 00077443A CO 5251460 A1 CO5251460 A1 CO 5251460A1
Authority
CO
Colombia
Prior art keywords
carbon atoms
alkyl
amino
optionally substituted
arylalkyl
Prior art date
Application number
CO00077443A
Other languages
English (en)
Inventor
Rainer Albert
Claus Ehrhardt
Hommel Ulrich
Jorg Kallen
Meingassner Josef Gottfried
Didier Roche
Wattanasin Sompong
Gabriele Weitz-Schmid
Karl 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 CO5251460A1 publication Critical patent/CO5251460A1/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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • 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
    • A61P9/10Drugs 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

Landscapes

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

Abstract

La presente invención se relaciona con un compuesto de la fórmula l:<EMI FILE="00077443_1" ID="1" IMF=JPEG >en donde:n es1, 2, ó 3, R1 es H, alquilo de 1 a 4 átomos de carbono; arilo; o arilalquilo de 1 a 4 átomos de carbono;Y es alquileno de 1 a 4 átomos de carbono; -CO-C-alquileno de 1 a 4 átomos de carbono; -CO-C-alquenileno de 2 a 5 átomos de carbono; -CO-NH-; -CO-C-alquileno de 1 a 3 átomos de carbono-NH-; ó -CO-O-,R2 es un residuo aromático o heteroaromático, cada uno opcionalmente sustituido por CF3, halógeno, OH, alcoxilo de 1 a 4 átomos de carbono, amino, amino sustituido por mono- o di-alquilo de 1 a 4 átomos de carbono, fenilo, bencilo, o alquilo de 1 a 4 átomos de carbono opcionalmente sustituido por amino,R3 es la cadena lateral presente sobre el Ca de un a-aminoácido,R4 es bifenililo; o bencilo, hidroxibencilo, a - ó ß-naf-tilmetilo, 5,6,7,8-tetrahidro-ß-naftilmetilo, o indolilmetilo, cada uno opcionalmente sustituido sobre el anillo por CF3, halógeno, OH, alcoxilo de 1 a 4 átomos de carbono, amino, amino sustituido por mono- o di-alquilo de 1 a 4 átomos de carbono, fenilo, bencilo, o alquilo de 1 a 4 átomos de carbono opcionalmente sustituido por amino, yX es -CN; -NR5R6; u -O-R8, en donde R5 es H, alquilo de 1 a 6 átomos de carbono, arilo, o arilalquilo de 1 a 4 átomos de carbono, R6 es H ó alquilo de 1 a 6 átomos de carbono, y R8 es H, alquilo de 1 a 4 átomos de carbono, arilo, o arilalquilo de 1 a 4 átomos de carbono, en forma libre o en forma de sal. Igualmente, se refiere al proceso para la preparación de dicho compuesto y a composiciones farmacéuticas que lo contienen.
CO00077443A 1999-10-13 2000-10-11 Diazepanes, proceso para su preparacion y composicion farmaceutica que los contiene CO5251460A1 (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
CO5251460A1 true CO5251460A1 (es) 2003-02-28

Family

ID=23651420

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00077443A CO5251460A1 (es) 1999-10-13 2000-10-11 Diazepanes, proceso para su preparacion y composicion farmaceutica que los contiene

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 (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6110922A (en) 1998-12-29 2000-08-29 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
CA2414461A1 (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
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
PE20020420A1 (es) 2000-10-02 2002-06-27 Novartis Ag Derivados de diazacicloalcanodiona como antagonistas del antigeno asociado a la funcion del linfocito-1 (lfa-1)
GB0301561D0 (en) * 2003-01-23 2003-02-26 Novartis Ag Organic compounds
TWI311557B (en) * 2003-01-23 2009-07-01 Novartis A Pharmaceutically active diazepanes
PL1682537T3 (pl) 2003-11-05 2012-09-28 Sarcode Bioscience Inc Modulatory adhezji komórkowej
WO2007054128A1 (en) * 2005-11-14 2007-05-18 Dominion Pharmakine S.L. Novel inhibitors of the lfa-1/icam-1 interaction, and uses thereof
GB0507918D0 (en) * 2005-04-19 2005-05-25 Novartis Ag Organic compounds
CA2609053C (en) 2005-05-17 2017-04-25 Sarcode Corporation Compositions and methods for treatment of eye disorders
EP3797775A1 (en) 2007-10-19 2021-03-31 Novartis AG 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
US8378105B2 (en) 2009-10-21 2013-02-19 Sarcode Bioscience Inc. Crystalline pharmaceutical and methods of preparation and use thereof
GB201016864D0 (en) 2010-10-06 2010-11-17 Univ Aston Therapeutic methods
CN104797574B (zh) 2012-07-25 2019-11-22 原生质生物科学股份有限公司 Lfa-1抑制剂及其多晶型物

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
WO1999020618A1 (en) * 1997-10-21 1999-04-29 Active Biotech Ab Thiadiazoles amides useful as antiinflammatory agents

Also Published As

Publication number Publication date
PE20010745A1 (es) 2001-07-17
CY1105020T1 (el) 2010-03-03
DE60025639D1 (de) 2006-04-06
EP1220852A1 (en) 2002-07-10
WO2001027102A1 (en) 2001-04-19
ECSP003707A (es) 2002-05-23
DE60025639T2 (de) 2006-11-16
EP1220852B1 (en) 2006-01-18
ES2257328T3 (es) 2006-08-01
DK1220852T3 (da) 2006-05-15
ATE316084T1 (de) 2006-02-15
JP3889623B2 (ja) 2007-03-07
AU7918500A (en) 2001-04-23
JP2003511447A (ja) 2003-03-25

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