CA2450740C - Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes - Google Patents

Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes Download PDF

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Publication number
CA2450740C
CA2450740C CA002450740A CA2450740A CA2450740C CA 2450740 C CA2450740 C CA 2450740C CA 002450740 A CA002450740 A CA 002450740A CA 2450740 A CA2450740 A CA 2450740A CA 2450740 C CA2450740 C CA 2450740C
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Prior art keywords
compound
6alkyl
treatment
effective amount
substituted
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Expired - Lifetime
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CA002450740A
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English (en)
French (fr)
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CA2450740A1 (en
Inventor
Scott D. Edmondson
Michael H. Fisher
Dooseop Kim
Malcolm Maccoss
Emma R. Parmee
Ann E. Weber
Jinyou Xu
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Merck Sharp and Dohme LLC
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Merck and Co Inc
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Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of CA2450740A1 publication Critical patent/CA2450740A1/en
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    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/28Insulins
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
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    • 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
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    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Communicable Diseases (AREA)
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  • Reproductive Health (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
CA002450740A 2001-07-06 2002-07-05 Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes Expired - Lifetime CA2450740C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30347401P 2001-07-06 2001-07-06
US60/303,474 2001-07-06
PCT/US2002/021349 WO2003004498A1 (en) 2001-07-06 2002-07-05 Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

Publications (2)

Publication Number Publication Date
CA2450740A1 CA2450740A1 (en) 2003-01-16
CA2450740C true CA2450740C (en) 2006-02-14

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CA002450740A Expired - Lifetime CA2450740C (en) 2001-07-06 2002-07-05 Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

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US (9) US6699871B2 (cg-RX-API-DMAC10.html)
EP (4) EP2226324A1 (cg-RX-API-DMAC10.html)
JP (1) JP3762407B2 (cg-RX-API-DMAC10.html)
KR (1) KR100606871B1 (cg-RX-API-DMAC10.html)
CN (2) CN1290848C (cg-RX-API-DMAC10.html)
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BE (1) BE2007C047I2 (cg-RX-API-DMAC10.html)
BG (1) BG108493A (cg-RX-API-DMAC10.html)
BR (1) BRPI0210866B8 (cg-RX-API-DMAC10.html)
CA (1) CA2450740C (cg-RX-API-DMAC10.html)
CR (1) CR7235A (cg-RX-API-DMAC10.html)
CY (3) CY2007019I2 (cg-RX-API-DMAC10.html)
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GE (2) GEP20053734B (cg-RX-API-DMAC10.html)
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PT (2) PT1412357E (cg-RX-API-DMAC10.html)
RS (1) RS50737B (cg-RX-API-DMAC10.html)
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