AR045536A1 - Inhibidores de la fosfodiesterasa tipo -iv - Google Patents

Inhibidores de la fosfodiesterasa tipo -iv

Info

Publication number
AR045536A1
AR045536A1 ARP040103114A ARP040103114A AR045536A1 AR 045536 A1 AR045536 A1 AR 045536A1 AR P040103114 A ARP040103114 A AR P040103114A AR P040103114 A ARP040103114 A AR P040103114A AR 045536 A1 AR045536 A1 AR 045536A1
Authority
AR
Argentina
Prior art keywords
ring
alkyl
heterocyclyl
nrxry
alkynyl
Prior art date
Application number
ARP040103114A
Other languages
English (en)
Inventor
Venkata P Palle
Sarala Balachandran
Mohammad Salman
Gagan Kukreja
Nidhi Gupta
Abhijit Ray
Sunanda G Dastidar
Original Assignee
Ranbaxy Lab Ltd
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 Ranbaxy Lab Ltd filed Critical Ranbaxy Lab Ltd
Publication of AR045536A1 publication Critical patent/AR045536A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • C07D498/10—Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Otolaryngology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se relaciona con derivados de isoxazolina, que puede ser utilizada como inhibidores selectivos de la fosfodiesterasa (PDE tipo IV. En especial, los compuestos revelados en la presente pueden ser útiles en el tratamiento del SIDA, asma, artritis, bronquitis, enfermedad pulmonar obstructiva crónica (COPD), psoriasis, rinitis alérgica, shock, dermatitis atópica, enfermedad de Crohn, síndrome de angustia respiratoria en adultos (ARDA), granuloma eosinofílico, conjuntivitis alérgica, osteoartritis, colitis ulcerosa y demás enfermedades inflamatorias en un paciente, especialmente en seres humanos. También se relaciona con procesos para la preparación de compuestos revelados, como asimismo composiciones farmacéuticas de los mismos, y su uso como inhibidores de la fosfodiesterasa (PDE) tipo IV. Reivindicación 1: Un compuesto que tiene la estructura de la fórmula (1), y sus sales farmacéuticamente aceptables, solvatos farmacéuticamente aceptables, enantiómeros, diastereómeros u óxidos-N, en donde: X es oxígeno; R1 es hidrógeno; alquilo; heterociclilo; (CH2)1-4OR', siempre y cuando R2 también sea (CH2)1-4OR'; -C(=O)NRxRy, siempre y cuando R2 también sea -C(=O)NRxRy; o -(CH2)mC(=O)R3; R2 es -(CH2)mC(=O)R3; - (CH2)1-4OR', siempre y cuando R1 también sea (CH2)1-4OR'; -C(=O)NRxRy siempre que R1 también sea -C(=O)NRxRy, o R1 y R2 juntos formen un anillo cicloalquilo o heterociclilo opcionalmente sustituido en donde el sustituyente opcional es oxo, alquilo, alquenilo, alquinilo, halógeno, nitro, -NH2, -C(=O)NRxRy, -NHCOOR6, ciano, hidroxi, alcoxi, o amino sustituido; R4 es hidrógeno; alquilo; -OR5; halógeno; -NH2, amino sustituido; ciano; carboxi; o -C(=O)NRxRy; o R2 y R4 forman el sistema de anillo monocíclico o bicíclico saturado o no saturado de 4-12 miembros opcionalmente sustituido fusionado al anillo B que tiene 0-4 heteroátomo(s) seleccionados del grupo que consiste de N, O y S, en donde los sustituyentes son uno o más de entre alquilo, halógeno, hidroxi, alcoxi, -NH2 o amino sustituido, con la salvedad de que R2 y R4 juntos no forman -CH2-O-CH2-O-CH2-; R7 es hidrógeno, alquilo, alquenilo, alquinilo, -OR5, halógeno, ciano, -NH2 o amino sustituido; X1 y X2 son cada uno independientemente hidrógeno, alquilo, alcarilo, cicloalquilo, heterociclilo, heteroarilo, heterociclilalquilo o heteroarilalquilo; Y es un átomo de oxígeno; un átomo de azufre; o -NR; Y1 y Y2 son cada uno independientemente hidrógeno; alquilo; -OR; -SR; o -NHR; en donde cualquiera de entre Y1 y X1 y X1 y Y2 juntos opcionalmente forman un anillo cíclico fusionado con el anillo A, conteniendo el anillo C3-5 dentro del anillo y que tiene 1-3 heteroátomos como ser N, O y S; X1 y X2 juntos opcionalmente forman un anillo cíclico fusionado con el anillo A, conteniendo el anillo C3-5 dentro del anillo y teniendo 2-3 heteroátomos como ser N, O y S, en donde el halógeno es F, Cl, Br, o I; R' es alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heterociclilo o heteroarilo saturado o no saturado; Rx y Ry son cada uno independientemente hidrógeno, alquilo, C3-6 alquenilo, C3-6 alquinilo, cicloalquilo, -SO2R5, arilo, alcarilo, heteroarilo, heterociclilo, heteroarilalquilo, y heterociclilalquilo; m es un entero entre 0-2; R3 es Rp o Rq opcionalmente sustituido; R6 es alquilo, alquenilo, alquinilo, cicloalquilo, alcarilo, heteroarilalquilo o heterociclilalquilo; y R es hidrógeno, acilo, arilo, o alquilo; y en donde R5 es hidrógeno, alquilo, alquenilo, alquinilo, arilo, cicloalquilo, alcarilo, heteroarilo, heteroarilalquilo, heterociclilo o heterociclilalquilo; Rp es un anillo heterociclilo o heteroarilo, en donde los anillos se adjuntan a (CH2)mC(=O) a través de N, y Rq es un anillo heterociclilo o heteroarilo en donde los mencionados anillos se ligan a -(CH2)mC(=O) a través de C.
ARP040103114A 2003-08-29 2004-08-30 Inhibidores de la fosfodiesterasa tipo -iv AR045536A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US49894703P 2003-08-29 2003-08-29

Publications (1)

Publication Number Publication Date
AR045536A1 true AR045536A1 (es) 2005-11-02

Family

ID=34272753

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103114A AR045536A1 (es) 2003-08-29 2004-08-30 Inhibidores de la fosfodiesterasa tipo -iv

Country Status (11)

Country Link
US (1) US7825147B2 (es)
EP (1) EP1663999A2 (es)
JP (1) JP2007504123A (es)
AR (1) AR045536A1 (es)
AU (1) AU2004268847A1 (es)
BR (1) BRPI0413330A (es)
CA (1) CA2537185A1 (es)
NZ (1) NZ545748A (es)
RU (1) RU2387646C2 (es)
WO (1) WO2005021515A2 (es)
ZA (1) ZA200602214B (es)

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RU2720203C1 (ru) 2017-01-20 2020-04-27 Пфайзер Инк. 1,1,1-трифтор-3-гидроксипропан-2-илкарбаматные производные как ингибиторы magl
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PL3638666T3 (pl) 2017-06-13 2022-01-03 Bayer Aktiengesellschaft Chwastobójczo skuteczne 3-fenyloizoksazolino-5-karboksyamidy amidów kwasu tetrahydro- i dihydrofuranokarboksylowego
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US7825147B2 (en) 2010-11-02
WO2005021515B1 (en) 2005-10-27
CA2537185A1 (en) 2005-03-10
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NZ545748A (en) 2010-03-26
AU2004268847A1 (en) 2005-03-10
ZA200602214B (en) 2007-04-25
US20050075383A1 (en) 2005-04-07
JP2007504123A (ja) 2007-03-01
BRPI0413330A (pt) 2006-10-10
EP1663999A2 (en) 2006-06-07

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