ECSP941066A - Derivados de 1.5 benzodiazepina - Google Patents

Derivados de 1.5 benzodiazepina

Info

Publication number
ECSP941066A
ECSP941066A EC1994001066A ECSP941066A ECSP941066A EC SP941066 A ECSP941066 A EC SP941066A EC 1994001066 A EC1994001066 A EC 1994001066A EC SP941066 A ECSP941066 A EC SP941066A EC SP941066 A ECSP941066 A EC SP941066A
Authority
EC
Ecuador
Prior art keywords
carbon atoms
alkyl
group
halogen
hydrogen
Prior art date
Application number
EC1994001066A
Other languages
English (en)
Inventor
Harry Finch
Pritom Shah
Carr Robin Arthur Ellis
Original Assignee
Glaxo Inc
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 Glaxo Inc filed Critical Glaxo Inc
Publication of ECSP941066A publication Critical patent/ECSP941066A/es

Links

Classifications

    • 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
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • 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
    • A61P1/16Drugs 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
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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
    • 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
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Compuesto de la fórmula general (I) (gráfico), y sales fisiológicas aceptables de los mismos, caracterizadas porque el grupo NR1R2 representa un anillo heterociclilo saturado de 5 a 7 miembros, el cual puede estar sustituido con uno o dos grupos metilo; R3 es un grupo alquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 6 átomos de carbono o fenilo opcionalmente sustituido con uno o dos átomos de halógeno; R4 es fenilo sustituido con uno o dos grupos que se seleccionan del grupo que consiste de halógeno, alquilo de 1 a 4 átomos de carbono, trifluorometilo, trifluorometoxi o (CH2)nR5 en donde n es cero o 1 y R5 representa un grupo alcoxi de 1 a 4 átomos de carbono, hidroxi, nitro, ciano, CO2R6, S(O)p CH3, NR7R8, CONR7R8, SO2NR7CO (alquilo de 1 a 4 átomos de carbono), tetrazolilo, carboxiamidotetrazolilo o 3-trifluorometil-1,2,4-triazolilo; R6 es hidrógeno, alquilo de 1 a 4 átomos de carbono o bencilo; R7 es hidrógeno o alquilo de 1 a 4 átomos de carbono, SO2CH3 o SO2CF3, X representa hidrógeno, un grupo de alquilo de 1 a 4 átomos de 1 a 4 átomos de carbono o halógeno; m es cer, 1 ó 2 y p es cero 1 ó 2.
EC1994001066A 1993-04-15 1994-04-12 Derivados de 1.5 benzodiazepina ECSP941066A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB939307833A GB9307833D0 (en) 1993-04-15 1993-04-15 Modulators of cholecystokinin and gastrin

Publications (1)

Publication Number Publication Date
ECSP941066A true ECSP941066A (es) 1994-11-16

Family

ID=10733915

Family Applications (1)

Application Number Title Priority Date Filing Date
EC1994001066A ECSP941066A (es) 1993-04-15 1994-04-12 Derivados de 1.5 benzodiazepina

Country Status (34)

Country Link
US (2) US5646140A (es)
EP (1) EP0694039B1 (es)
JP (1) JP3406317B2 (es)
KR (1) KR100364948B1 (es)
CN (1) CN1058487C (es)
AP (2) AP512A (es)
AT (1) ATE198894T1 (es)
AU (1) AU681139B2 (es)
CA (1) CA2158973C (es)
CZ (1) CZ286695B6 (es)
DE (1) DE69426624T2 (es)
DK (1) DK0694039T3 (es)
EC (1) ECSP941066A (es)
ES (1) ES2154674T3 (es)
FI (1) FI954853A0 (es)
GB (1) GB9307833D0 (es)
GR (1) GR3035641T3 (es)
HK (1) HK1003943A1 (es)
HU (1) HU223467B1 (es)
IL (2) IL109315A0 (es)
IS (2) IS4147A (es)
MY (2) MY131569A (es)
NO (1) NO311133B1 (es)
NZ (1) NZ265272A (es)
OA (1) OA10355A (es)
PE (2) PE50594A1 (es)
PH (1) PH30897A (es)
PL (1) PL178790B1 (es)
PT (1) PT694039E (es)
RU (1) RU2135486C1 (es)
SK (1) SK281211B6 (es)
TW (1) TW487703B (es)
WO (1) WO1994024149A1 (es)
ZA (2) ZA942571B (es)

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US5739129A (en) * 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
CA2186900A1 (en) * 1994-04-14 1995-10-26 Christopher Joseph Aquino Cck or gastrin modulating 5-heterocyclic-1,5-benzodiazepines
EP0755394A1 (en) * 1994-04-15 1997-01-29 Glaxo Wellcome Inc. A method of inducing cholecystokinin agonist activity using 1,4-benzodiazepine compounds
PE27497A1 (es) * 1994-04-15 1997-08-07 Glaxo Inc Derivados de 1,5 benzodiazepina
GB9420747D0 (en) * 1994-10-14 1994-11-30 Glaxo Inc 1,5 benzodiazepine derivatives
US5910495A (en) * 1994-10-14 1999-06-08 Glaxo Wellcome Inc. Use of 1,5-benzo b!1,4-diazepines to control gastric emptying
GB9420763D0 (en) * 1994-10-14 1994-11-30 Glaxo Inc Acetamide derivatives
US5780464A (en) * 1994-10-14 1998-07-14 Glaxo Wellcome Inc. Enteric coated compositions of 1,5-benzodiazepine derivatives having CCK antagonistic or agonistic activity
GB9420748D0 (en) * 1994-10-14 1994-11-30 Glaxo Inc 1,5 benzodiazepine derivatives
US5750353A (en) * 1995-12-11 1998-05-12 New England Medical Center Hospitals, Inc. Assay for non-peptide agonists to peptide hormone receptors
IL124808A0 (en) 1995-12-11 1999-01-26 New England Medical Center Inc Assay for and uses of peptide hormone receptor ligands
PT945445E (pt) * 1996-12-10 2004-01-30 Zeria Pharm Co Ltd Derivados de 1,5-benzodiazepina
CA2283564C (en) 1997-04-15 2007-07-10 Csir Pharmaceutical compositions having appetite suppressant activity
AR022044A1 (es) * 1999-05-06 2002-09-04 Glaxo Group Ltd Derivados de 1,5-benzodiazepina
GB2355657B (en) 1999-10-27 2004-07-28 Phytopharm Plc Inhibitors Of Gastric Acid Secretion
GB2363985B (en) 2000-06-30 2004-09-29 Phytopharm Plc Extracts,compounds & pharmaceutical compositions having anti-diabetic activity and their use
US6768024B1 (en) 2000-08-04 2004-07-27 Lion Bioscience Ag Triamine derivative melanocortin receptor ligands and methods of using same
US20020180095A1 (en) * 2001-05-29 2002-12-05 Berard Steven O. Thermally conductive carbon fiber extrusion compounder and method of using same
US7074805B2 (en) * 2002-02-20 2006-07-11 Abbott Laboratories Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
CA2476936A1 (en) * 2002-02-20 2003-08-28 Chih-Hung Lee Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor
US6933311B2 (en) * 2003-02-11 2005-08-23 Abbott Laboratories Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
US7015233B2 (en) * 2003-06-12 2006-03-21 Abbott Laboratories Fused compounds that inhibit vanilloid subtype 1 (VR1) receptor
EA010888B1 (ru) * 2004-05-25 2008-12-30 Пфайзер Продактс, Инк. Тетраазабензо[е]азуленовые производные и их аналоги
CN1333077C (zh) * 2005-04-15 2007-08-22 华南农业大学 缩胆囊素活性片段的串联表达及其应用
EP2054390B1 (en) * 2006-08-25 2012-04-11 Abbott Laboratories Indazole derivatives that inhibit trpv1 and uses thereof
JP2010513557A (ja) 2006-12-20 2010-04-30 アボット・ラボラトリーズ 疼痛治療のためのtrpv1バニロイド受容体アンタゴニストとしてのn−(5,6,7,8−テトラヒドロナフタレン−1−イル)尿素誘導体および関連化合物
EP2489660A1 (en) * 2008-03-20 2012-08-22 Abbott Laboratories Methods for making central nervous system agents that are TRPV1 antagonists
CN103102285B (zh) * 2013-01-30 2015-07-29 淮阴师范学院 对氨基苯乙腈的制备方法
EP3071205B1 (en) 2013-11-18 2020-02-05 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
LT3071203T (lt) 2013-11-18 2021-05-25 Forma Therapeutics, Inc. Tetrahidrochinolino kompozicijos kaip bet bromodomeno inhibitoriai
MX2018000916A (es) 2015-07-22 2018-09-05 Enanta Pharm Inc Derivados de benzodiazepina como inhibidores de rsv.
SG10201913587WA (en) 2016-02-05 2020-02-27 Denali Therapeutics Inc Inhibitors of receptor-interacting protein kinase 1
ES2912295T3 (es) 2016-12-09 2022-05-25 Denali Therapeutics Inc Compuestos útiles como inhibidores de RIPK1
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FR2641280B1 (fr) * 1988-12-29 1994-01-21 Roussel Uclaf Nouveaux derives de la 2,4-dioxo 2,3,4,5-tetrahydro 1h-1,5-benzodiazepine, leur procede de preparation et leur application comme medicaments
FR2659653B1 (fr) * 1990-03-13 1992-05-22 Rhone Poulenc Sante Derives de l'uree, leur preparation et les medicaments les contenant.
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CA2186900A1 (en) * 1994-04-14 1995-10-26 Christopher Joseph Aquino Cck or gastrin modulating 5-heterocyclic-1,5-benzodiazepines

Also Published As

Publication number Publication date
SK125395A3 (en) 1996-06-05
AU6567694A (en) 1994-11-08
IL109316A (en) 1999-03-12
NO954090D0 (no) 1995-10-13
CN1120843A (zh) 1996-04-17
US5646140A (en) 1997-07-08
FI954853A (fi) 1995-10-12
US5585376A (en) 1996-12-17
RU2135486C1 (ru) 1999-08-27
DE69426624T2 (de) 2001-06-21
CA2158973C (en) 2006-06-06
GR3035641T3 (en) 2001-06-29
HU9502978D0 (en) 1995-12-28
DK0694039T3 (da) 2001-05-21
EP0694039B1 (en) 2001-01-24
CZ286695B6 (en) 2000-06-14
NZ265272A (en) 1997-07-27
ZA942571B (en) 1994-11-11
IL109316A0 (en) 1994-07-31
FI954853A0 (fi) 1995-10-12
KR100364948B1 (ko) 2003-03-29
AP462A (en) 1996-02-19
PE50994A1 (es) 1995-01-06
AP9400635A0 (en) 1994-04-30
ZA942570B (en) 1994-11-11
PH30897A (en) 1997-12-23
NO311133B1 (no) 2001-10-15
CZ267595A3 (en) 1996-04-17
HK1003943A1 (en) 1998-11-13
CA2158973A1 (en) 1994-10-27
EP0694039A1 (en) 1996-01-31
HU223467B1 (hu) 2004-07-28
ES2154674T3 (es) 2001-04-16
PL178790B1 (pl) 2000-06-30
HUT74102A (en) 1996-11-28
AP512A (en) 1996-07-29
ATE198894T1 (de) 2001-02-15
AP9400634A0 (en) 1994-04-30
JP3406317B2 (ja) 2003-05-12
AU681139B2 (en) 1997-08-21
CN1058487C (zh) 2000-11-15
TW487703B (en) 2002-05-21
PL311084A1 (en) 1996-02-05
PE50594A1 (es) 1995-01-06
GB9307833D0 (en) 1993-06-02
IS4147A (is) 1994-10-16
IS4148A (is) 1994-10-16
PT694039E (pt) 2001-06-29
NO954090L (no) 1995-12-13
IL109315A0 (en) 1994-07-31
DE69426624D1 (de) 2001-03-01
WO1994024149A1 (en) 1994-10-27
JPH08508744A (ja) 1996-09-17
MY131569A (en) 2007-08-30
SK281211B6 (sk) 2001-01-18
OA10355A (en) 2001-10-19
MY112237A (en) 2001-05-31

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