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CO5261629A1 - ARYLOXYACETIC ACIDS FOR DIABETES AND LIPID DISORDERS - Google Patents

ARYLOXYACETIC ACIDS FOR DIABETES AND LIPID DISORDERS

Info

Publication number
CO5261629A1
CO5261629A1 CO01011989A CO01011989A CO5261629A1 CO 5261629 A1 CO5261629 A1 CO 5261629A1 CO 01011989 A CO01011989 A CO 01011989A CO 01011989 A CO01011989 A CO 01011989A CO 5261629 A1 CO5261629 A1 CO 5261629A1
Authority
CO
Colombia
Prior art keywords
alkyl
alkenyl
group
alkynyl
cycloalkyl
Prior art date
Application number
CO01011989A
Other languages
Spanish (es)
Inventor
Liu Kun
Xu Libo
Siliphaivanh Phieng
A Brian Jones
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of CO5261629A1 publication Critical patent/CO5261629A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/04Drugs 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P35/00Antineoplastic 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto que tiene la Fórmula I: <EMI FILE="01011989_1" ID="1" IMF=JPEG >y las sales y precursores de drogas farmacéuticamente aceptables de éste, en dondeR1 y R2 son cada uno independientemente seleccionados del grupo conformado por H, F, alquil C1-5, alquenil C2-5, y alquinil C2-5, en donde dichos grupos alquil, alquenil, y alquinil pueden ser lineales ó ramificados y van opcionalmente sustituidos con 1-3 átomos de halógeno; u opcionalmente R1 y R2 juntos forman un cicloalquil C3-6;R3 y R4 son cada uno independientemente seleccionados del grupo conformado por alquil C1-5, alquenil C2-5, alquinil C2-5, y cloro, a condición de que R3 y R4 no sean ambos cloro, en donde dichos grupos alquil, alquenil, y alquinil pueden ser lineales ó ramificados y van opcionalmente sustituidos con 1-5 átomos de flúor;X es N ó CR; Y es O, S, ó NR; Z es O ó S;Cada R es independientemente seleccionado del grupo conformado por H, alquil C1-5, alquenil C2-5, y alquinil C2-5, en donde dichos alquil, alquenil, y alquinil pueden ser lineales ó ramificados y van opcionalmente sustituidos con 1-5 átomos de flúor y/o con un grupo -O-alquil C1-3, en donde dicho grupo -O-alquil C1-3 se encuentra opcionalmente sustituido con 1-7 átomos de flúor; yR5 se selecciona del grupo conformado por H, alquil C1-6, alquenil C2-6, alquinil C2-6, Aril C6-10, -O-alquil C1-6, -O-alquenil C2-6, -O-alquinil C2-6, -O-Aril C6-10, Cicloalquil C3-6, Heterociclil de 5-6 miembros, Heteroaril de 5-6 miembros, -O-Cicloalquil C3-6, -O-Heterociclil de 5-6 miembros, -O-Heteroaril de 5-6 miembros, y un grupo alquil C1-4 el cual comprende en una posición que interrumpe la cadena, ó al final de la cadena, un grupo seleccionado entre Aril C6-10, Cicloalquil C3-6, Heterociclil de 5-6 miembros, y Heteroaril de 5-6 miembros, en donde cada uno de dichos grupos alquil, alquenil, alquinil, -O-alquil, -O-alquenil, y -O-alquinil es lineal o ramificado y va opcionalmente sustituido con 1-5 átomos de flúor y/o con un grupo -OCH3 ó -OCF3, y cada uno de dichos grupos Aril, Cicloalquil, Heteroaril, Heterociclil, -O-Aril, -O-Cicloalquil, -O-Heteroaril, y -O-Heterociclil va opcionalmente sustituido con 1-7 átomos de halógeno y/o con un grupo -OCH3 ó -OCF3.A compound having Formula I: <EMI FILE = "01011989_1" ID = "1" MFI = JPEG> and pharmaceutically acceptable drug salts and precursors thereof, where R1 and R2 are each independently selected from the group consisting of H , F, C1-5 alkyl, C2-5 alkenyl, and C2-5 alkynyl, wherein said alkyl, alkenyl, and alkynyl groups can be linear or branched and are optionally substituted with 1-3 halogen atoms; or optionally R1 and R2 together form a C3-6 cycloalkyl; R3 and R4 are each independently selected from the group consisting of C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, and chlorine, provided that R3 and R4 they are not both chlorine, wherein said alkyl, alkenyl, and alkynyl groups can be linear or branched and are optionally substituted with 1-5 fluorine atoms, X is N or CR; Y is O, S, or NR; Z is O or S; Each R is independently selected from the group consisting of H, C1-5 alkyl, C2-5 alkenyl, and C2-5 alkynyl, wherein said alkyl, alkenyl, and alkynyl can be linear or branched and optionally go substituted with 1-5 fluorine atoms and / or with a -O-C1-3 alkyl group, wherein said -O-C1-3 alkyl group is optionally substituted with 1-7 fluorine atoms; and R5 is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, -O-C1-6 alkyl, -O-C2-6 alkenyl, -O-C2 alkynyl -6, -O-C6-10 aryl, C3-6 cycloalkyl, 5-6 membered heterocyclyl, 5-6 membered heteroaryl, -O-C3-6 cycloalkyl, 5-6 membered -O-heterocyclyl, -O - 5-6-member heteroaryl, and a C1-4 alkyl group which comprises in a position that disrupts the chain, or at the end of the chain, a group selected from Aril C6-10, C3-6 cycloalkyl, 5-heterocyclyl -6 members, and 5-6-member heteroaryl, wherein each of said alkyl, alkenyl, alkynyl, -O-alkyl, -O-alkenyl, and -O-alkynyl groups is linear or branched and is optionally substituted with 1 -5 fluorine atoms and / or with a group -OCH3 or -OCF3, and each of said groups Aril, Cycloalkyl, Heteroaryl, Heterocyclyl, -O-Aryl, -O-Cycloalkyl, -O-Heteroaryl, and -O- Heterocyclyl is optionally substituted with 1-7 halogen atoms and / or with a group -OCH3 or -OCF3.

CO01011989A 2000-02-18 2001-02-15 ARYLOXYACETIC ACIDS FOR DIABETES AND LIPID DISORDERS CO5261629A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US18359300P 2000-02-18 2000-02-18

Publications (1)

Publication Number Publication Date
CO5261629A1 true CO5261629A1 (en) 2003-03-31

Family

ID=22673475

Family Applications (1)

Application Number Title Priority Date Filing Date
CO01011989A CO5261629A1 (en) 2000-02-18 2001-02-15 ARYLOXYACETIC ACIDS FOR DIABETES AND LIPID DISORDERS

Country Status (7)

Country Link
EP (1) EP1259494A4 (en)
JP (1) JP2003523336A (en)
AU (1) AU784722B2 (en)
CA (1) CA2400021A1 (en)
CO (1) CO5261629A1 (en)
PE (1) PE20011056A1 (en)
WO (1) WO2001060807A1 (en)

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