[go: up one dir, main page]

AR037950A1 - Compuestos de succinimida heterociclicos, fusionados y analogos de los mismos, moduladores de la funcion del receptor de la hormona nuclear - Google Patents

Compuestos de succinimida heterociclicos, fusionados y analogos de los mismos, moduladores de la funcion del receptor de la hormona nuclear

Info

Publication number
AR037950A1
AR037950A1 ARP020105038A ARP020105038A AR037950A1 AR 037950 A1 AR037950 A1 AR 037950A1 AR P020105038 A ARP020105038 A AR P020105038A AR P020105038 A ARP020105038 A AR P020105038A AR 037950 A1 AR037950 A1 AR 037950A1
Authority
AR
Argentina
Prior art keywords
substituted
cycloalkenyl
cycloalkyl
alkyl
heterocycle
Prior art date
Application number
ARP020105038A
Other languages
English (en)
Inventor
Mark E Salvati
James Aaron Balog
Dacia A Pickering
Soren Giese
Aberra Fura
Ramesh N Patel
Ronald L Hanson
Jacques Y Roberge
James R Corte
Steven H Spergel
Raj Misra
Hai-Yun Xiao
Wenying Li
Toomas Mitt
Richard A Rampulla
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR037950A1 publication Critical patent/AR037950A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/18—Bridged 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P3/06—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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Addiction (AREA)
  • Nutrition Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Método de preparación y método de uso de tales compuestos en el tratamiento de condiciones asociados con el receptor de la hormona nuclear tal como el cáncer y padecimientos inmunes, y composiciones farmacéuticas que contienen tales compuestos. Reivindicación 1: Un compuesto de la siguiente fórmula (1), en donde los símbolos tienen los siguientes significados y son, cada vez que se presentan, seleccionados independientemente: G es un grupo arilo o heterociclo, donde el grupo es mono- o policíclico, y el cual está opcionalmente sustituido en una o más posiciones; Z1 es O, S, NH, o NR6; Z2 es O, S, NH, o NR6; A1 es CR7 o N; A2 es CR7 o N; Y es J-J'-J'' donde J es (CR7R7')n y n=0-3, J' es un enlace u O, S, S=O, SO2, NH, NR7, CR7R7', R2P=O, R2P=S, R2OP=O, R2NHP=O, OP=OOR2, OP=ONHR2, OSO2, NHNH, NHNR6, NR6NH, N=N, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, o heterociclo o heterociclo sustituido, y J'' es (CR7R7')n y n=0-3, donde Y no es enlace; y W' es CR7CR7'-CR7C7', CR7R7'-C=O, C=O-C=O, CR7R7'-C=CH2, C=CH2-C=CH2, CR7R7'-C=NR1, C=NR1-C=NR1, NR9-CR7R7', N=CR8, N=N, NR9-NR9', cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, o arilo o arilo sustituido, en donde cuando W' no es NR9-CR7R7', N=CR8, N=N, NR9-NR9', o heterociclo o heterociclo sustituido, entonces J' deberá ser O, S, S=O, SO2, NH, NR7, OP=OOR2, OP=ONHR2, OSO2, NHNH, NHNR6, NR6NH, o N=N; cuando W es CR7R7'-CR7R7', los sustituyentes R7 y R7', cada que se presentan, pueden tomarse juntos para formar un sistema de anillo heterocíclico sustituido o no sustituido o carbocíclico sustituido o no sustituido que puede formarse por cualquier combinación de R7 y R7' enlazado al mismo átomo de carbono; Q1 es H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilalquilo o arilalquilo sustituido, alquinilo o alquinilo sustituido, arilo o arilo sustituido, heterociclo (por ejemplo heteroarilo) o heterociclo sustituido (por ejemplo heteroarilo), halo, CN, R1OC=O, R4C=O, R5R6NC=O, HOCR7R7', nitro, R1OCH2, R1O, NH2, C=OSR1, SO2R1 o NR4R5; Q2 es H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilalquilo o arilalquilo sustituido, alquinilo o alquinilo sustituido, arilo o arilo sustituido, heterociclo (por ejemplo heteroarilo) o heterociclo sustituido (por ejemplo heteroarilo sustituido), halo, CN, R1OC=O, R4C=O, R5R6NC=O, HOCR7R7', nitro, R1OCH2, R1O, NH2, C=OSR1, SO2R1, o NR4R5; L es un enlace, (CR7R7')n, NH, NR5, NH(CR7R7')n, o NR5(CR7R7')n, donde n=0-3; R1 y R1' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido; R2 es alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido; R3 y R3' con cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, halo, CN, hidroxilamina, hidroxamida, alcoxi o alcoxi sustituido, amino, NR1R2, tiol, alquiltio o alquiltio sustituido; R4 es H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, R1C=O, R1OC=O, R1NHC=O, SO2OR1, o SO2R1, SO2NR1R1'; R5 es alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, R1C=O, R1NHC=O, SO2R1, SO2OR1, o SO2NR1R1'; R6 es alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, CN, OH, OR1, R1C=O, R1NHC=O, SO2R1, SO2OR1, o SO2NR1R1'; R7 y R7' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, halo, CN, OR4, nitro, hidroxilamina, hidroxamida, amino, NHR4, NR2R5, NR5R5, NOR1, tiol, alquiltio o alquiltio sustituido, HOC=O, R1C=O, R1(C=O)O, R1OC=O, R1NHC=O, NH2C=O, SO2R1, SOR1, PO3R1R1', R1R1'NC=O, C=OSR1, SO2R1, SO2OR1, o SO2NR1R1', o, en donde A1 o A2 contiene un grupo R7 y W contiene un grupo R7, los grupos R7 de A1 o A2 y W forman juntos un anillo heterocíclico; R8 y R8' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, nitro, halo, CN, OR1, amino, NHR4, NR2R5, NOR1, alquiltio o alquiltio sustituido, C=OSR1, R1OC=O, R1C=O, R1NHC=O, R1R1'NC=O, SO2OR1, S=OR1, SO2R1, PO3R1R1', o SO2NR1R1'; R9 y R9' son cada uno independientemente H, alquilo o alquilo sustituido, alquenilo o alquenilo sustituido, alquinilo o alquinilo sustituido, cicloalquilo o cicloalquilo sustituido, cicloalquenilo o cicloalquenilo sustituido, heterociclo o heterociclo sustituido, cicloalquilalquilo o cicloalquilalquilo sustituido, cicloalquenilalquilo o cicloalquenilalquilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido, arilo o arilo sustituido, arilalquilo o arilalquilo sustituido, CN, OH, OR1, R1C=O, R1OC=O, R1NHC=O, SO2R1, SO2OR1, o SO2NR1R1'; con la condición de que: (1) cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es -CH2-CH2-, y A1 y A2 son CH, entonces G-L no es fenilo, fenilo monosustituido o fenilo que está sustituido con dos o más de los siguientes grupos: metoxi, halo, NO2, metilo, CH3-S-, OH, CO2H, trifluorometilo, -C(O)-C6H5, NH2, 4-7-epoxi, hexahidro-1H-isoindol-1,3(2H)diona, o -C(O)-CH3; (2) cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es CH2-CH2, y uno de A1 y A2 es CH y el otro es CR7, entonces G-L no es fenilo no sustituido; (3) cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es CH2-CH2, y uno de A1 y A2 es CH y el otro es C-CH3, entonces G-L no es fenilo sustituido con cloro y/o metilo; (4) cuando Y' es -O- o -S-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es CH2-CH2, y uno de A1 y A2 es CH y el otro es CH o C-alquilo, entonces G-L no es piperazin-alquilo N-sustituido o imidazolidin-alquilo N-sustituido; (5) cuando Y' es -O-; Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W'es CH2-CH2, y A1 y A2 son CH, entonces G-L no es oxazol o triazol; (6) cuando Y' es -O-; Q1 y Q2 son hidrógeno o metilo, Z1 y Z2 son O, W' es CH2-CH2, y A1 y A2 son CH o C-CH3, entonces G-L no es tiazol o tiazol sustituido; (7) cuando Y' contiene un grupo J' seleccionado de S, S=O, SO2, NH, NR7, R2P=O, R2P=S, R2OP=O, R2NHP=O, OP=OOR2, OP=ONHR2, OSO2, NHNH, NHR6, NR6NH o N=N, W' es CR7R7'-CR7R7', y Z1 y Z2 son O, entonces G-L no es fenilo no sustituido; (8) cuando y es NR7, W' es fenilo no sustituido o sustituido, y Q1 y Q2 son hidrógeno, entonces Z1 Y Z2 no son O; (9)cuando Y' es -O-, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es dihidroisoxazol que porta un grupo fenilo opcionalmente sustituido, A1 y A2 son CH, entonces G-L no es fenilo no sustituido o diclorofenilo; (10) cuando Y' es O, Q1 y Q2 son hidrógeno, Z1 y Z2 son O, W' es óxido de etileno, y A1 y A2 son CH, entonces G-L no es metilfenilo o clorofenilo; (11) cuando Y' es NR7-CR7R7', W' es CR8=CR8', Q1 y Q2 son hidrógeno, A1 y A2 son CH, C-CH3, -C-CH2-
ARP020105038A 2001-12-19 2002-12-19 Compuestos de succinimida heterociclicos, fusionados y analogos de los mismos, moduladores de la funcion del receptor de la hormona nuclear AR037950A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US2511601A 2001-12-19 2001-12-19

Publications (1)

Publication Number Publication Date
AR037950A1 true AR037950A1 (es) 2004-12-22

Family

ID=27609007

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020105038A AR037950A1 (es) 2001-12-19 2002-12-19 Compuestos de succinimida heterociclicos, fusionados y analogos de los mismos, moduladores de la funcion del receptor de la hormona nuclear

Country Status (31)

Country Link
EP (1) EP1458723B1 (es)
JP (1) JP2005523257A (es)
KR (1) KR20040086248A (es)
CN (1) CN1589271A (es)
AR (1) AR037950A1 (es)
AT (1) ATE411319T1 (es)
AU (1) AU2002361785B2 (es)
BR (1) BR0215281A (es)
CA (1) CA2471342A1 (es)
CO (1) CO5640082A2 (es)
DE (1) DE60229435D1 (es)
DK (1) DK1458723T3 (es)
ES (1) ES2314127T3 (es)
GE (1) GEP20063817B (es)
HR (1) HRP20040567A2 (es)
HU (1) HUP0402554A3 (es)
IL (1) IL162547A0 (es)
IS (1) IS7324A (es)
MX (1) MXPA04005876A (es)
NO (1) NO20043068L (es)
NZ (1) NZ533471A (es)
PL (1) PL370904A1 (es)
PT (1) PT1458723E (es)
RU (1) RU2330038C2 (es)
SI (1) SI1458723T1 (es)
TW (1) TWI263640B (es)
UA (1) UA78265C2 (es)
UY (1) UY27595A1 (es)
WO (1) WO2003062241A1 (es)
YU (1) YU53604A (es)
ZA (1) ZA200404812B (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040077605A1 (en) 2001-06-20 2004-04-22 Salvati Mark E. Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
EP1467979B1 (en) 2001-12-19 2008-08-13 Bristol-Myers Squibb Company Fused heterocyclic compounds and analogs thereof modulators of nuclear hormone receptor function
US7202264B2 (en) 2003-01-31 2007-04-10 Isis Pharmaceuticals, Inc. Supports for oligomer synthesis
FR2860793A1 (fr) * 2003-10-14 2005-04-15 Entomed Composes derives de norcantharidine, leurs procedes de preparation, les compositions les contenant et leurs utilisations
EP1692139B1 (en) * 2003-11-13 2013-02-13 Isis Pharmaceuticals, Inc. 5,6 -dihydroxy-isoindole derivatives as linkers for oligomer solid phase synthesis
US7605264B2 (en) 2004-01-16 2009-10-20 Bristol-Myers Squibb Company Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7326728B2 (en) 2004-01-16 2008-02-05 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κβ activity and use thereof
US7625921B2 (en) 2004-01-16 2009-12-01 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7569689B2 (en) 2004-01-16 2009-08-04 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7253283B2 (en) 2004-01-16 2007-08-07 Bristol-Myers Squibb Company Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7273881B2 (en) 2004-01-16 2007-09-25 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
AU2005223481A1 (en) * 2004-03-17 2005-09-29 Pfizer Products Inc. Novel benzyl(idene)-lactam derivatives
US7317024B2 (en) 2005-01-13 2008-01-08 Bristol-Myers Squibb Co. Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7642273B2 (en) 2005-01-13 2010-01-05 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7411071B2 (en) 2005-01-13 2008-08-12 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7361654B2 (en) 2005-01-13 2008-04-22 Bristol-Myers Squibb Co. Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
ES2349476T3 (es) * 2005-09-09 2011-01-03 Schering Corporation Nuevos derivados de 4-ciano, 4-amino y 4-aminometilo de compuestos de pirazolo[1,5-a]piridinas, pirazolo[1,5-c]pirimidinas y 2h-indazol y derivados de 5-ciano, 5-amino y 5-aminometilo de compuestos de imidazo[1,2-a]piridinas e imidazo[1,5-a]pirazinas, como inhibidores de cinasa dependiente de ciclina.
WO2008042571A2 (en) 2006-09-29 2008-04-10 Smithkline Beecham Corporation Substituted indole compounds
WO2008157291A2 (en) * 2007-06-15 2008-12-24 Bristol-Myers Squibb Company CRYSTALLINE FORMS OF (3Aα, 4β, 5α, 7β, 7Aα)-4-(OCTAHYDRO-5-ETHYLSULFONAMIDO-4,7-DIMETHYL-1,3-DIOXO-4,7-EPOXY-2H-ISOINDOL-2-YL)-2-(TRIFLUOROMETHYL)BENZONITRILE AND METHOD OF PREPARATION
AU2010242307A1 (en) * 2009-04-30 2011-11-24 Sumitomo Chemical Company, Limited Thiophene derivative
WO2011007819A1 (ja) 2009-07-17 2011-01-20 塩野義製薬株式会社 ラクタムまたはベンゼンスルホンアミド化合物を含有する医薬
EP2475366A1 (en) 2009-09-11 2012-07-18 Bayer Pharma Aktiengesellschaft Substituted (heteroarylmethyl) thiohydantoins as anticancer drugs
LT2523731T (lt) 2010-01-14 2019-02-11 Novartis Ag Antinksčių hormoną modifikuojančio agento panaudojimas
WO2014111871A1 (en) 2013-01-17 2014-07-24 Aurigene Discovery Technologies Limited 4,5-dihydroisoxazole derivatives as nampt inhibitors
WO2014179564A1 (en) * 2013-05-01 2014-11-06 Vitae Pharmaceuticals, Inc. Thiazalopyrrolidine inhibitors of ror-gamma
JP6156074B2 (ja) * 2013-11-08 2017-07-05 住友化学株式会社 スクシンイミド化合物及びその用途
SG11201606080SA (en) 2014-02-03 2016-08-30 Vitae Pharmaceuticals Inc Dihydropyrrolopyridine inhibitors of ror-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
EA201892486A1 (ru) * 2014-12-19 2019-07-31 Арагон Фармасьютикалз, Инк. Способ получения соединения диарилтиогидантоина
WO2016118666A1 (en) * 2015-01-20 2016-07-28 Arvinas, Inc. Compounds and methods for the targeted degradation of the androgen receptor
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US10301261B2 (en) 2015-08-05 2019-05-28 Vitae Pharmaceuticals, Llc Substituted indoles as modulators of ROR-gamma
EP3377482B1 (en) 2015-11-20 2021-05-12 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
WO2018122317A1 (en) 2016-12-29 2018-07-05 Enyo Pharma Thiophene derivatives as antiviral agents
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
MA49685A (fr) 2017-07-24 2021-04-14 Vitae Pharmaceuticals Llc INHIBITEURS DE ROR gamma
EP4121044A4 (en) * 2020-03-20 2024-03-13 University Of Southern California ANDROGEN RECEPTOR REGULATION BY SMALL MOLECULE ENANTIOMERS
EP4146348B1 (en) 2020-05-08 2024-07-03 Halia Therapeutics, Inc. Inhibitors of nek7 kinase
CN114848795B (zh) * 2021-02-03 2023-04-14 四川大学 RORa蛋白及其激动剂在制备抗衰老药物中的应用
US20250064948A1 (en) * 2022-02-14 2025-02-27 The Johns Hopkins University Gcpii inhibition for the treatment of sarcopenia and aging
WO2024059200A1 (en) 2022-09-14 2024-03-21 Halia Therapeutics, Inc. Nek7 inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3320270A (en) * 1963-10-08 1967-05-16 Tri Kem Corp Certain 2-acylimidothiazole compounds
US3215597A (en) * 1963-10-30 1965-11-02 Dow Chemical Co Methods and compositions for use in animal husbandry
US3261845A (en) * 1964-07-14 1966-07-19 Dow Chemical Co N-phenyl derivatives of 3,6-epoxyhexahydrophthalimide
US4892943A (en) * 1985-10-16 1990-01-09 American Home Products Corporation Fused bicyclic imides with psychotropic activity
JPS63170383A (ja) * 1987-02-26 1988-07-14 Nippon Zeon Co Ltd 脂環式ジカルボン酸イミド化合物
EP0497843A4 (en) * 1989-10-27 1992-09-23 The Du Pont Merck Pharmaceutical Company (n-phthalimidoalkyl) piperidines
CN1103769C (zh) * 1996-10-25 2003-03-26 第一制药株式会社 三环胺衍生物
FR2764890B1 (fr) * 1997-06-24 1999-08-27 Adir Nouveaux derives chromeniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE69910432D1 (de) * 1998-12-22 2003-09-18 Lilly Co Eli Substituierte pyrroloindole
US6521753B1 (en) * 2000-05-31 2003-02-18 Johnson & Johnson Vision Care, Inc. Indolinospiropyran compounds and methods for their manufacture
BR0111298A (pt) * 2000-06-28 2005-05-10 Bristol Myers Squibb Co Moduladores seletivos dos receptores de andrógenos e métodos para identificação, projeto e uso dos mesmos
NZ524803A (en) * 2000-09-19 2004-09-24 Bristol Myers Squibb Co Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function

Also Published As

Publication number Publication date
KR20040086248A (ko) 2004-10-08
PL370904A1 (en) 2005-05-30
AU2002361785B2 (en) 2008-05-22
TW200304810A (en) 2003-10-16
UY27595A1 (es) 2003-07-31
HUP0402554A2 (hu) 2005-03-29
HRP20040567A2 (en) 2005-06-30
RU2330038C2 (ru) 2008-07-27
WO2003062241A1 (en) 2003-07-31
ATE411319T1 (de) 2008-10-15
GEP20063817B (en) 2006-05-10
CA2471342A1 (en) 2003-07-31
DK1458723T3 (da) 2009-02-09
CN1589271A (zh) 2005-03-02
IL162547A0 (en) 2005-11-20
TWI263640B (en) 2006-10-11
HUP0402554A3 (en) 2009-01-28
UA78265C2 (en) 2007-03-15
NZ533471A (en) 2007-05-31
ES2314127T3 (es) 2009-03-16
CO5640082A2 (es) 2006-05-31
MXPA04005876A (es) 2005-05-16
DE60229435D1 (de) 2008-11-27
PT1458723E (pt) 2008-12-26
SI1458723T1 (sl) 2009-02-28
JP2005523257A (ja) 2005-08-04
NO20043068L (no) 2004-09-08
EP1458723A4 (en) 2005-12-21
WO2003062241A8 (en) 2004-10-21
RU2004122403A (ru) 2005-05-27
EP1458723A1 (en) 2004-09-22
YU53604A (sh) 2006-08-17
BR0215281A (pt) 2004-10-19
EP1458723B1 (en) 2008-10-15
ZA200404812B (en) 2005-08-26
IS7324A (is) 2004-06-18

Similar Documents

Publication Publication Date Title
AR037950A1 (es) Compuestos de succinimida heterociclicos, fusionados y analogos de los mismos, moduladores de la funcion del receptor de la hormona nuclear
AR035340A1 (es) Compuestos de succinimida heterociclicos fusionados y analogos de los mismos, las composiciones farmaceuticas que los contienen y metodos para preparar dichos compuestos
MX2020011501A (es) Compuestos novedosos.
ES2080919T3 (es) Nuevos derivados de bencimidazol y de azabencimidazol, antagonistas de los receptores al tromboxano, sus procedimientos de preparacion, intermediarios de sintesis, composiciones que los contienen.
CA2423103A1 (en) N-acylsulfonamide apoptosis promoters
CO5590957A2 (es) Amino-1,3,5-triazinas sustituidas en n con radicales biciclicos quirales, procedimiento para su preparacion, composiciones de las mismas y su uso como herbicidas y reguladores del crecimiento de las plantas
AR032453A1 (es) Derivados alquinil fenil heteroaromaticos activadores de glucoquinasa, un proceso para su preparacion, composiciones farmaceuticas, el uso de dichos derivados para la preparacion de medicamentos
ES2572189T3 (es) Derivados de 2,3-dihidroimidazo[1,2-c]quinazolina sustituidos de utilidad en el tratamiento de trastornos hiperproliferativos y enfermedades asociadas con la angiogénesis
IL68969A0 (en) Urea derivatives,their preparation and herbicidal and plant growth inhibition compositions containing them
AR040076A1 (es) Derivados de piridazin-3(2h)-ona
AR071959A1 (es) Derivado de benceno o tiofeno y su uso como inhibidor de vap-1
RU2011137457A (ru) Пестицыдные композиции
AR019790A2 (es) Compuestos derivados de la eritromicina, composiciones que los contienen. uso para preparar un medicamento
AR040031A1 (es) Compuestos de pirazol-pirimidina anilina utiles como inhibidores de cinasa y composiciones farmaceuticas que los contienen
DK0794949T3 (da) Hidtil ukendte 3,5-dioxo-(2H,4H)-1,2,4-triazinderivater, fremstilling heraf og deres anvendelse som lægemidler
MX9203249A (es) Derivados del acido bencimidazolin-2-oxo-1-carboxilico y composiciones farmaceuticas que los contienen.
RU2010101004A (ru) Новые микробиоциды
AR043959A1 (es) Derivados de indolona-acetamida, procesos para prepararlos, composiciones farmaceuticas que los contienen y su uso como productos farmaceuticos
MX9202438A (es) Esteroides 3-carboxi insaturados substituidos en la posicion 17 beta, procedimiento para su preparacion y composicion farmaceutica que los contiene.
MX2010001673A (es) Mejoramientos en o relacionados a compuestos organicos.
CO5550397A2 (es) Orto-ciclopropil-tienil-carboxamidas con actividad fungicida
ES369934A1 (es) Un procedimiento de preparacion de derivados 3-alcoxi-tia- nifteno-2 - carboxamidas sustituidas.
HU901366D0 (en) Fungicidal compositions comprising substituted oximethers and process for preparation of the active ingredients
AR053326A1 (es) 4 - feniltetrahidroisoquinolinas sustituidas, su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la activacion de nhe y composicion farmaceutica que las comprende.
DK627088A (da) Forbindelser beslaegtet med avermectiner og milbemyciner, antiparasitiske praeparater indeholdende disse og fremgangsmaade til bekaempelse af parasitangreb

Legal Events

Date Code Title Description
FB Suspension of granting procedure