AR045503A1 - Un derivado de isoxazolina como un inhibidor contra varias caspasas, un procedimiento para preparar el mismo y una composicion terapeutica para prevenir l a inflamacion y la apoptosis que comprende al mismo - Google Patents

Un derivado de isoxazolina como un inhibidor contra varias caspasas, un procedimiento para preparar el mismo y una composicion terapeutica para prevenir l a inflamacion y la apoptosis que comprende al mismo

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Publication number
AR045503A1
AR045503A1 ARP040103065A ARP040103065A AR045503A1 AR 045503 A1 AR045503 A1 AR 045503A1 AR P040103065 A ARP040103065 A AR P040103065A AR P040103065 A ARP040103065 A AR P040103065A AR 045503 A1 AR045503 A1 AR 045503A1
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Argentina
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sac
scac
compound
formula
exist
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ARP040103065A
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English (en)
Inventor
Min-Jung Kim
Jung-Gyu Park
Hee-Dong Park
Kyeong-Sik Min
Tae-Soo Lee
Sang-Kyun Lee
Soo-Hyeon Kim
Hee-Kyung Jeong
Sun-Hwa Lee
Hwa-Dong Kim
Ae-Ri Kim
Ki-Sook Park
Hyun-Ik Shin
Hyeong-Wook Choi
Kyu-Woong Lee
Jae-Hoon Lee
Tae-Ho Heo
Ho-Jun Kim
Tae-Sik Kwon
Hye-Kyung Chang
Yeong-Soo Oh
Cheol-Won Park
Yong-Jin Jang
Tae-Kyo Park
Sung-Sub Kim
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Lg Life Sciences Ltd
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Publication of AR045503A1 publication Critical patent/AR045503A1/es

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    • 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
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    • 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
    • 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
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/28—Drugs 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/04—Antibacterial 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
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  • Communicable Diseases (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (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)

Abstract

La presente se refiere a un derivado de isoxazolina como un inhibidor contra varias caspasas, a un procedimiento para preparar el mismo y a una composición terapéutica para prevenir la inflamación y la apoptosis que comprende al mismo. Reivindicación 1: Un compuesto de la fórmula (1), caracterizado porque: I) R representa H, una cadena alquilo simple (-SAC), una cadena cicloalquilo simple (-SCAC), un grupo arilo (-Ar), o una cadena alquilo simple sustituida por arilo (-SAC- Ar), II) R1 representa -SAC, -SCAC, -Ar, -SAC-Ar, o un residuo de cadena lateral de todos los aminoácidos naturales; y el compuesto de fórmula (1), puede existir en una forma diastereomérica específica, o mezclas de las mismas, cuando el carbono al cual está unido R1 se convierte en un estereocentro debido al grupo R1; o el compuesto de fórmula (1) puede tener un grupo protector en forma de éster (-CO2R3, en donde R3 es -SAC) o en forma de sulfonamida (-CONHSO2R4 en donde R4 es -SAC), o puede existir en forma de una sal farmacéuticamente aceptable, cuando R1 es un residuo de cadena lateral de un aminoácido que contiene una parte carboxilo; o el compuesto de fórmula (1) también puede existir en forma de una sal farmacéuticamente aceptable cuando R1 es un residuo de cadena lateral de un aminoácido que contiene una parte de base, III) R2 representa -SAC, -SCAC, -Ar, -SAC-Ar, o un residuo de cadena lateral de los aminoácidos; y el compuesto de fórmula (1) puede existir en una forma diastereomérica específica, o mezclas de las mismas, cuando el carbono al cual está unido R2 se convierte en un estereocentro debido al grupo R2; o el compuesto de fórmula (1) puede tener un grupo protector en forma de éster (-CO2R5, en donde R5 es - SAC) o en forma de sulfonamida (-CONHSO2R6, en donde R6 es -SAC), o puede existir en forma de una sal farmacéuticamente aceptable, cuando R2 es un residuo de cadena lateral de un aminoácido que contiene una parte carboxilo; o el compuesto de fórmula (1) también puede existir en la forma de una sal farmacéuticamente aceptable cuando R2 es un residuo de cadena lateral de un aminoácido que contiene una parte de base, o R2 representa además H; -(CH2)nOR7 en donde R7 es -SAC, -SCAC, -Ar, o -SAC-Ar y n = 1 ó 2; o -(CH2)nOC(=O)R8 en donde R8 es -SAC, -SCAC, -Ar, o -SAC-Ar y n = 1 ó 2, IV) A representa -(CH2)n- (n = 0-4), -O-(CH2)n- (n = 0-4) o -NR9-(CH2)n- (n = 0-4) en donde R9 es -SAC, -SCAC, -Ar, o -SAC-Ar, V) B representa H, -SAC, -SCAC, -Ar, o -SAC-Ar, o VI) R y R1 pueden formar un ciclo junto con el átomo de carbono al cual están unidos, en donde -R-R1- es -(CH2)n-, -(CH2)n-O-(CH2)m, o -(CH2)n-NR10-(CH2)m- en donde n + m < 9 y R10 es -SAC, -SCAC, -Ar, -SAC-Ar, -C(=O)-SAC, -C(=O)-SAC, - C(=O)-Ar, o -C(=O)-SAC-Ar, VII) X representa -C(=O)CH2OR11, en donde R11 es -SAC, -SCAC, -Ar, o -SAC-Ar; -C(=O)CH2OC(=O)R12 en donde R12 es -SAC, -SCAC, -Ar o -SAC-Ar; -CH=CH-CO2R13 en donde R13 es -SAC, -SCAC, -Ar o -SAC-Ar; -CH=CH-SO2R14 en donde R14 es -SAC, -SCAC, -Ar o -SAC-Ar; -C(=O)CH=CH2; o -COCH2-W en donde W es -N2, -F, -Cl, -Br, -I, -NR15R16 (R15 y R16 son cada uno -SAC, -SCAC, -Ar, o -SAC-Ar, o juntos pueden formar un grupo cíclico saturado o insaturado de 3 a 6 miembros), -SR17 (R17 es -SAC, -SCAC, -Ar o -SAC-Ar) o es el grupo de fórmulas (2), en donde: Y es H, -OH, -OR18 (R18 = -SAC o -SCAC), -C(=O)R19 (R19 = -H, -SAC, o -SCAC), -F, -Cl, -Br, -I, -CN, -NC, -N3, -CO2H, CF3, -CO2R20 (R20 = -SAC o -SCAC), -C(=O)NHR21 (R21 = - SAC o -SCAC), o -C(=O)NR22R23 (R22 y R23 son cada uno -SAC, -SCAC, -Ar, o -SAC-Ar), R24 es H, -SAC, -SAC-Ar o -Ar, una sal, o un estereoisómero del mismo.
ARP040103065A 2003-08-27 2004-08-26 Un derivado de isoxazolina como un inhibidor contra varias caspasas, un procedimiento para preparar el mismo y una composicion terapeutica para prevenir l a inflamacion y la apoptosis que comprende al mismo AR045503A1 (es)

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KR20030059451 2003-08-27

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AR045503A1 true AR045503A1 (es) 2005-11-02

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US (1) US7557133B2 (es)
EP (1) EP1660464B1 (es)
JP (1) JP4503017B2 (es)
KR (1) KR100594544B1 (es)
CN (1) CN1842521B (es)
AP (1) AP2104A (es)
AR (1) AR045503A1 (es)
BR (1) BRPI0413848B8 (es)
CA (1) CA2535711C (es)
EA (1) EA012080B1 (es)
EC (1) ECSP066378A (es)
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MA (1) MA27999A1 (es)
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