PE20090897A1 - Compuestos de biciclolactama sustituida como inhibidores de la enzima dgat-1 - Google Patents

Compuestos de biciclolactama sustituida como inhibidores de la enzima dgat-1

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Publication number
PE20090897A1
PE20090897A1 PE2008001299A PE2008001299A PE20090897A1 PE 20090897 A1 PE20090897 A1 PE 20090897A1 PE 2008001299 A PE2008001299 A PE 2008001299A PE 2008001299 A PE2008001299 A PE 2008001299A PE 20090897 A1 PE20090897 A1 PE 20090897A1
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PE
Peru
Prior art keywords
alkyl
dgat
dihydropyrimide
oxazepin
perfluoroalkyl
Prior art date
Application number
PE2008001299A
Other languages
English (en)
Inventor
Robert Lee Dow
Michael John Munchhof
Original Assignee
Pfizer Prod 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.)
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Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of PE20090897A1 publication Critical patent/PE20090897A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

REFERIDO A UN COMPUESTO DERRIVADO DE BICICLOLACTAMA DE FORMULA (1), DONDE R1 ES H, -ALQUILO (C1-C4), -PERFLUOROALQUILO(C1-C4), -PERFLUOROALCOXI(C1-C4) O -ALCOXI(C1-C4); R2 Y R3 SON CADA UNO H, -ALQUILO(C1-C4) O -PERFLUOROALQUILO(C1-C4); O R2 Y R3 JUNTOS CON EL CARBONO AL CUAL ESTAN UNIDOS FORMAN CICLOALQUILO(C3-C6); R4 ES H O -ALQUILO(C1-C4); R5a, R5b, R5c Y R5d SON CADA UNO H, F, -ALQUILO(C1-C4), ENTRE OTROS; Q ES -O- o UN ENLACE; A ES -CICLOALQUILENO(C3-C6), -CICLOALQUENILENO(C3-C6) O FENILENO; Z ES -C(R6a)(R6b) O UN ENLACE, DONDE R6a Y R6b SON CADA UNO -H O -ALQUILO(C1-C4) O R6a Y R6b, TOMADOS JUNTO CON EL CARBONO AL QUE ESTAN UNIDOS, ES UN CICLOALQUILO (C3-C6); R7 ES C(O)R8, CIANO, HIDROXILO, ENTRE OTROS; R8 ES -OR9 O NHR10; R9 ES -H, -ALQUILO(C1-C4) O PERFLUOROALQUILO(C1-C4) Y R10 ES -H, -ALQUILO(C1-C4), TETRAZOLILO O S(O)2CF3. SON COMPUESTOS PREFERIDOS: {TRANS-4-[4-(4-CLORO-5-OXO-7,8-DIHIDROPIRIMIDO[5,4-f][1,4]OXAZEPIN-6-(5H)-IL)FENIL]CICLOHEXIL}ACETATO DE METILO, 2-((1S,4S)-4-(4-((R)-4-CLORO-8-METIL-5-OXO-7,8-DIHIDROPIRIMIDO-[5,4-f][1,4]OXAZEPIN-6(5H)-IL)FENIL)CICLOHEXIL)ACETATO DE METILO, (TRANS-4-{4-[(7S)-4-CLORO-7-METIL-5-OXO-7,8-DIHIDROPIRIMIDO[5,4-f][1,4]OXAZEPIN-6(5H)-IL]FENIL}CICLOHEXIL)ACETATO DE METILO ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A UN METODO DE PREPARACION. DICHO COMPUESTO TIENE ACTIVIDAD INHIBITORIA SOBRE DGAT-1(DIACILGLICEROL O-ACILTRANSFERASA) Y ES UTIL EN EL TRATAMIENTO DE LA OBESIDAD, DIABETES TIPO 2, ENTRE OTROS
PE2008001299A 2007-08-02 2008-08-01 Compuestos de biciclolactama sustituida como inhibidores de la enzima dgat-1 PE20090897A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US95350707P 2007-08-02 2007-08-02

Publications (1)

Publication Number Publication Date
PE20090897A1 true PE20090897A1 (es) 2009-08-06

Family

ID=39926534

Family Applications (1)

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PE2008001299A PE20090897A1 (es) 2007-08-02 2008-08-01 Compuestos de biciclolactama sustituida como inhibidores de la enzima dgat-1

Country Status (34)

Country Link
US (2) US20090036425A1 (es)
EP (1) EP2185567B1 (es)
JP (1) JP4629808B2 (es)
KR (1) KR20100032443A (es)
CN (1) CN101772504A (es)
AP (1) AP2010005163A0 (es)
AR (1) AR067780A1 (es)
AT (1) ATE502948T1 (es)
AU (1) AU2008281545B2 (es)
BR (1) BRPI0815067A2 (es)
CA (1) CA2695291C (es)
CL (1) CL2008002227A1 (es)
CO (1) CO6251365A2 (es)
CR (1) CR11223A (es)
CY (1) CY1111628T1 (es)
DE (1) DE602008005757D1 (es)
DK (1) DK2185567T3 (es)
DO (1) DOP2010000046A (es)
EA (1) EA201000050A1 (es)
EC (1) ECSP109932A (es)
ES (1) ES2361716T3 (es)
HN (1) HN2008001191A (es)
HR (1) HRP20110335T1 (es)
MA (1) MA31580B1 (es)
PA (1) PA8791601A1 (es)
PE (1) PE20090897A1 (es)
PL (1) PL2185567T3 (es)
PT (1) PT2185567E (es)
SI (1) SI2185567T1 (es)
TN (1) TN2010000053A1 (es)
TW (1) TWI356059B (es)
UA (1) UA94833C2 (es)
WO (1) WO2009016462A2 (es)
ZA (1) ZA201000255B (es)

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