AR011092A1 - A COMPOUND DERIVED FROM TIAZOL BENZENSULFONAMIDES AS BETA3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY, A PHARMACEUTICAL COMPOSITION THAT IT UNDERSTANDS AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT. - Google Patents

A COMPOUND DERIVED FROM TIAZOL BENZENSULFONAMIDES AS BETA3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY, A PHARMACEUTICAL COMPOSITION THAT IT UNDERSTANDS AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT.

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Publication number
AR011092A1
AR011092A1 ARP980100357A ARP980100357A AR011092A1 AR 011092 A1 AR011092 A1 AR 011092A1 AR P980100357 A ARP980100357 A AR P980100357A AR P980100357 A ARP980100357 A AR P980100357A AR 011092 A1 AR011092 A1 AR 011092A1
Authority
AR
Argentina
Prior art keywords
compounds
treatment
obesity
diabetes
sulfur
Prior art date
Application number
ARP980100357A
Other languages
Spanish (es)
Original Assignee
Merck & Co 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
Priority claimed from GBGB9705041.3A external-priority patent/GB9705041D0/en
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR011092A1 publication Critical patent/AR011092A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Las bencensulfonamidas tiazol-substituidas que comprende la formula I donde: X es (1) un enlace, (2) alquileno C1-C3, opcionalmente substituido con1 o 2 grupos seleccionados entre metilo y halogeno, (3) alquileno C1-C3, donde dicho alquileno contiene un oxígeno, opcionalemnte con 1 o 2 gruposseleccionados de metilo y halogeno; m es 0 a 5; A es (1) fenilo, (2)un anillo heterocíclico de 5 a 6 miembros con desde 1 a 4 heteroátomos seleccionado deoxígeno, azufre y nitrogeno, (3) un anillo benceno fusionado a un anillo carboxílico C5-C10, (4) un anillo heterocíclico de 5 a 6 miembros con desde 1a 4 heteroátomos seleccionado de oxigeno, azufre y nitrogeno o, (5) un anillo heterocíclico de 5 o 6 miembros con desde 1 a 4 heteroátomos seleccionado deoxigeno , azufre y nitrogeno fusionado a un anillo carboxílico C5-C10; R1 es (1) alquilo C1-C10 opcionalmente sustituido con hasta 5 grupos como se defineen la memoria descriptiva, son agonistas receptores beta3 adrenérgicos conmuy poca actividad receptora beta1 y beta2 adrenérgica y como tales los compuestosson capaces de aumentar la lipolisis y el gasto de energía en las células. Los compuestos tienen por lo tanto una potente actividad para el tratamiento deobesidad ydiabetes de tipo II. Los compuestos también pueden usarse para disminuir los niveles de triglicéridos y los niveles de colesterol o paraelevar los niveles de lipoproteína de alta densidad o para disminuir la motilidad intestinal. Ademáslos compuestos pueden usarse para reducirinflamacion neurogenica o como agentes antidepresivos. Los compuestos se preparan mediante acoplamiento substituido. se describen las composicionesfarmacéuticas y usos de dichos compuestos para la manufactura de un medicamento para usar en el tratamiento para usar en el tratamiento de diabetes y obesidadThe thiazole-substituted benzenesulfonamides comprising formula I where: X is (1) a bond, (2) C1-C3 alkylene, optionally substituted with 1 or 2 groups selected from methyl and halogen, (3) C1-C3 alkylene, where said alkylene contains an oxygen, optionally with 1 or 2 selected groups of methyl and halogen; m is 0 to 5; A is (1) phenyl, (2) a 5- to 6-membered heterocyclic ring with from 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen, (3) a benzene ring fused to a C5-C10 carboxylic ring, (4) a 5- to 6-membered heterocyclic ring with from 1 to 4 heteroatoms selected from oxygen, sulfur, and nitrogen, or (5) a 5- or 6-membered heterocyclic ring with from 1 to 4 heteroatoms selected from deoxygen, sulfur, and nitrogen fused to a C5 carboxylic ring -C10; R1 is (1) C1-C10 alkyl optionally substituted with up to 5 groups as defined in the specification, they are beta3 adrenergic receptor agonists with little beta1 and beta2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in the cells. The compounds therefore have potent activity for the treatment of obesity and type II diabetes. The compounds can also be used to lower triglyceride levels and cholesterol levels or to raise high-density lipoprotein levels or to decrease intestinal motility. In addition, the compounds can be used to reduce neurogenic inflammation or as antidepressant agents. The compounds are prepared by substituted coupling. The pharmaceutical compositions and uses of said compounds for the manufacture of a medicament for use in treatment for use in the treatment of diabetes and obesity are described.

ARP980100357A 1997-01-28 1998-01-27 A COMPOUND DERIVED FROM TIAZOL BENZENSULFONAMIDES AS BETA3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY, A PHARMACEUTICAL COMPOSITION THAT IT UNDERSTANDS AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT. AR011092A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3676097P 1997-01-28 1997-01-28
GBGB9705041.3A GB9705041D0 (en) 1997-03-12 1997-03-12 Thiazole benzenesulfonamides as selective B3 agonists for the treatment of diabetes and obesity

Publications (1)

Publication Number Publication Date
AR011092A1 true AR011092A1 (en) 2000-08-02

Family

ID=26311166

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980100357A AR011092A1 (en) 1997-01-28 1998-01-27 A COMPOUND DERIVED FROM TIAZOL BENZENSULFONAMIDES AS BETA3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY, A PHARMACEUTICAL COMPOSITION THAT IT UNDERSTANDS AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT.

Country Status (22)

Country Link
EP (1) EP0968209A1 (en)
JP (1) JP2001509166A (en)
KR (1) KR20000070568A (en)
CN (1) CN1251099A (en)
AR (1) AR011092A1 (en)
AU (1) AU728812B2 (en)
BG (1) BG103686A (en)
BR (1) BR9807096A (en)
CA (1) CA2278739A1 (en)
EA (1) EA199900692A1 (en)
EE (1) EE9900328A (en)
HR (1) HRP980044A2 (en)
HU (1) HUP0002053A3 (en)
ID (1) ID22273A (en)
IL (1) IL131130A0 (en)
IS (1) IS5131A (en)
NO (1) NO993646L (en)
PE (1) PE52299A1 (en)
PL (1) PL334833A1 (en)
SK (1) SK100099A3 (en)
TR (1) TR199902442T2 (en)
WO (1) WO1998032753A1 (en)

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Also Published As

Publication number Publication date
AU728812B2 (en) 2001-01-18
CA2278739A1 (en) 1998-07-30
NO993646L (en) 1999-09-27
IS5131A (en) 1999-07-23
ID22273A (en) 1999-09-23
TR199902442T2 (en) 2000-07-21
BG103686A (en) 2000-06-30
PL334833A1 (en) 2000-03-27
EE9900328A (en) 2000-02-15
CN1251099A (en) 2000-04-19
HUP0002053A3 (en) 2001-09-28
WO1998032753A1 (en) 1998-07-30
BR9807096A (en) 2000-04-18
PE52299A1 (en) 1999-05-26
EP0968209A1 (en) 2000-01-05
KR20000070568A (en) 2000-11-25
JP2001509166A (en) 2001-07-10
NO993646D0 (en) 1999-07-27
AU6038498A (en) 1998-08-18
IL131130A0 (en) 2001-01-28
EA199900692A1 (en) 2000-02-28
SK100099A3 (en) 2000-05-16
HUP0002053A2 (en) 2001-08-28
HRP980044A2 (en) 1998-10-31

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