AR072185A1 - Agonistas de receptores s1p1 y uso de los mismos - Google Patents

Agonistas de receptores s1p1 y uso de los mismos

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Publication number
AR072185A1
AR072185A1 ARP090102221A ARP090102221A AR072185A1 AR 072185 A1 AR072185 A1 AR 072185A1 AR P090102221 A ARP090102221 A AR P090102221A AR P090102221 A ARP090102221 A AR P090102221A AR 072185 A1 AR072185 A1 AR 072185A1
Authority
AR
Argentina
Prior art keywords
alkyl
haloalkyl
substituted
cr10r10
formula
Prior art date
Application number
ARP090102221A
Other languages
English (en)
Inventor
Kelvin K C Sham
Victor J Cee
Brian Alan Lanman
Anthony B Reed
Susana C Neira
Michael J Frohn
Original Assignee
Amgen 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.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of AR072185A1 publication Critical patent/AR072185A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • 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
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A61P7/06—Antianaemics
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)

Abstract

La presente se refiere a compuestos que tienen actividad como agentes moduladores del receptor S1P, m s espec¡ficamente a compuestos que son agonistas del receptor S1P1. La presente tambien se refiere al uso de dichos compuestos para tratar enfermedades asociadas con la actividad inapropiada del receptor S1P1, tales como enfermedades autoinmunes. Reivindicacion 1: Un compuesto de formula (1) en donde m es 0, 1, 2 o 3; n es 0, 1, 2 o 3; o es 0, 1, 2 o 3; A es un fenilo, heterociclilo, cicloalquilo de tres a seis miembros, o un anillo heteroarilo de cinco o seis miembros; L es un anillo saturado de 3, 4, 5, 6 o 7 miembros que contiene 0, 1 o 2  tomos seleccionados de N, O y S y que opcionalmente contiene un doble enlace, estando sustituido el anillo por 0, 1 o 2 grupos seleccionados de F, Cl, alquilo C1-4, haloalquilo C1-4, OH, alquilo-O C1-4, y haloalquilo-O C1-4 X1 es N o CH; X2 es N o CH; X5 es N o CH; el grupo de formula (2) se selecciona entre los compuestos de formula (3), (4), (5), (6), (7), (8) y (9); R1 se selecciona de F, Cl, alquilo C1-4, haloalquilo C1-4, OH, alquilo-O C1-4, y haloalquilo-O C1-4; R2 se selecciona de F, Cl, alquilo C1-4, haloalquilo C1-4, OH, alquilo-O C1-4, y haloalquilo-O C1-4, R3 se selecciona de F, Cl, alquilo C1-4, haloalquilo C1-4, OH, alquilo-O C1-4, amino y haloalquilo-O C1-4; Z es: (i) un cicloalquilo sustituido con un grupo amino, monoalquilamino o dialquilamino; un cicloalquilalquilo sustituido con uno o dos grupos carboxi; un grupo amino monosustituido, amino disustituido, carboxialquilamino, hidroxialquilo, hidroxialquilo sustituido, hidroxialcoxi, hidroxialcoxi sustituido, aminoalquilo, aminoalcoxi, carboxialquilo, carboxialquilo sustituido, carboxialquiloxi, carboxialquiloxi sustituido, carboxialcoxialquilo, carboxialcoxialquilo sustituido, aminocarbonilo, acilamino, sulfonilamino, heterocicloamino, heterocicloaminoalquilo, heterocicloaminocarbonilo, heterocicloaminoxi, o heteroaralquilo; (ii) un grupo de formula (10) donde: q es 0, 1 o 2; R4 se selecciona de H, haloalquilo C1-3, alquilo C1-6; R5 se selecciona de H, haloalquilo C1-3, alquilo C1-4; o R4 y R5 junto con el  tomo de carbono al cual est n unidos forman un anillo carboc¡clico de 3, 4, 5, 6 o 7 miembros sustituido por 0, 1 o 2 grupos seleccionados de F, CI, alquilo C1-4, haloalquilo C1-4, OH, alquilo-O C1-4, y haloalquilo-O C1-4; R6 es un par solitario de electrones o O; R7 es H o alquilo C1-6; R8 se selecciona de H, F, Cl, alquilo C1-4, haloalquilo C1-4, OH, alquilo-O C1-4, y haloalquilo-O C1-4 o R7 y R8, cuando se toman juntos, forman un grupo que se selecciona de -(CR10R10)-, -(CR10R10)O-, -O(CR10R10)-, -(CR10R10)(CR10R10)-, y -(CR10R10)3-; R9 se selecciona de H, F, haloalquilo C1-3, alquilo C1-4, OH y alquilo-O C1-4; o R8 y R9 junto con el  tomo de carbono al cual est n unidos forman cicloalquilo; y cada R10 es independientemente en cada instancia seleccionado a partir de H, F, CI, alquilo C1-4, haloalquilo C1-4, OH, alquilo-O C1-4, y haloalquilo-O C1-4 o (iii) cuando R3 est  sobre un  tomo de carbono del anillo fenilo que es adyacente al carbono del anillo fenilo que est  unido a Z, entonces R3 y Z pueden combinarse para formar -CH=CH-NR11, -(CH2)2NR11-, -CH2NR11CH2-, -(CH2)2NR11CH2-, -N=CR11-NH-, o -N=CH-NR11-, donde R11 se selecciona de hidrogeno, hidroxialquilo, aminoalquilo, carboxialquilo, hidroxialquilo sustituido, carboxialquilo sustituido, o aminocarbonilo; o una farmaceuticamente aceptable del mismo; siempre que cuando el compuesto de formula (2) se selecciona de los compuestos de formula (6), (7), (8) y (9), entonces al menos uno de X1, X2 y X5 es N.
ARP090102221A 2008-06-20 2009-06-18 Agonistas de receptores s1p1 y uso de los mismos AR072185A1 (es)

Applications Claiming Priority (1)

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US7447608P 2008-06-20 2008-06-20

Publications (1)

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AR072185A1 true AR072185A1 (es) 2010-08-11

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ARP090102221A AR072185A1 (es) 2008-06-20 2009-06-18 Agonistas de receptores s1p1 y uso de los mismos

Country Status (10)

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US (2) US20120129828A1 (es)
EP (1) EP2306994B1 (es)
JP (1) JP5571073B2 (es)
AR (1) AR072185A1 (es)
AU (1) AU2009260726B2 (es)
CA (1) CA2728046A1 (es)
ES (1) ES2433579T3 (es)
MX (1) MX2010013555A (es)
TW (1) TW201000099A (es)
WO (2) WO2009154780A1 (es)

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US20120129828A1 (en) 2012-05-24
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US20100029611A1 (en) 2010-02-04
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US7842685B2 (en) 2010-11-30
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AU2009260726A1 (en) 2009-12-23
ES2433579T3 (es) 2013-12-11

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