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AR073821A1 - Derivados de 2-amidotiadiazol, agonistas de los receptores s1p1 - Google Patents

Derivados de 2-amidotiadiazol, agonistas de los receptores s1p1

Info

Publication number
AR073821A1
AR073821A1 ARP090103915A ARP090103915A AR073821A1 AR 073821 A1 AR073821 A1 AR 073821A1 AR P090103915 A ARP090103915 A AR P090103915A AR P090103915 A ARP090103915 A AR P090103915A AR 073821 A1 AR073821 A1 AR 073821A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
optionally substituted
hydrogen atom
groups
Prior art date
Application number
ARP090103915A
Other languages
English (en)
Inventor
Poveda Pedro Manuel Grima
Izquierdo Nuria Aguilar
Cepeda Marta Mir
Martinez Manuel Lopez
Original Assignee
Almirall Sa
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 Almirall Sa filed Critical Almirall Sa
Publication of AR073821A1 publication Critical patent/AR073821A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Derivados de 2-amidotiadiazol que tienen la estructura química representada por la formula (1) o sales o N-oxidos de los mismos farmacéuticamente aceptables, R1 representa: un grupo heteroarilo que contiene N, bicíclico de 8 a 10 miembros, opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halogeno, grupos hidroxicarbonilo, grupos alquilo C1-4, haloalquilo C1-4, alcoxi C1-4 y cicloalquilo C3-4; un grupo piridilo sustituido con uno o más sustituyentes seleccionados de átomos de halogeno, grupos hidroxi, hidroxicarbonilo, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, cicloalquilo C3-4 y grupos NR'R'', donde R' representa un átomo de hidrogeno o un grupo alquilo C1-4 y R'' representa un átomo de hidrogeno o un grupo alquilo C1-4 opcionalmente sustituido con un grupo hidroxi; un grupo piridona sustituido con uno o más sustituyentes seleccionados de átomos de halogeno, alquilo C1-4 y grupos haloalquilo C1-4, o un grupo de formula (2) donde Ra representa un átomo de hidrogeno o un grupo alquilo C1-4, Rb representa un átomo de hidrogeno, átomo de halogeno o grupo alquilo C1-4, Rd representa un átomo de hidrogeno, un grupo alquilo C1-4 o un grupo cicloalquilo C3-4, Rc representa un grupo hidroxi, alcoxi C1-4 que está opcionalmente sustituido con uno o más sustituyentes seleccionados de grupos hidroxi, alcoxi C1-3, grupos hidroxicarbonilo, alcoxi C1-4 carbonilo y grupos NHR4, donde R4 representa un átomo de hidrogeno; o Rc es un grupo acilo C2-4 o un grupo alquilo C1-4 opcionalmente sustituido con un grupo hidroxicarbonilo, o Rc representa -(CH2)(0-4)-L-R5 donde L representa -C(O)O-, -C(O)NH-, -S(O)2NH-, -NH-, -CONHS(O)2- o un grupo de formula (3) donde n y m independientemente son numeros enteros de 1 a 2, y R5 representa un átomo de hidrogeno o un grupo alquilo C1-4 opcionalmente sustituido con un grupo hidroxicarbonilo; R2 representa: un grupo arilo C5-10 monocíclico o bicíclico opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halogeno, alquilo C1-4, alcoxi C1-4 y grupos fenilo, donde el grupo alquilo está opcionalmente sustituido con uno o más átomos de halogeno; un grupo heteroarilo de 5-10 miembros monocíclico o bicíclico que comprende uno o más heteroátomos seleccionados de N, S y O opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halogeno, alquilo C1-4 y alcoxi C1-4, donde el grupo alquilo C1-4 está opcionalmente sustituido con uno o más átomos de halogeno; un grupo dihidrobenzodioxina o un grupo bencilo que está opcionalmente sustituido con uno o más sustituyentes seleccionados de átomos de halogeno; y R3 representa un grupo alquilo C1-6 lineal o ramificado, cicloalquil C3-6-alquilo C1-4, alcoxi C1-4-alquilo C1-4, un grupo di-alquilamino-alquilo C1-4, o un grupo fenil-alquilo C1-4; con la condicion de que cuando Rc representa un grupo metoxi o etoxi, entonces uno de Rb o Rd no puede ser un átomo de hidrogeno; con la condicion adicional de que el compuesto de formula (1) no es N-metil-N-(5-(6-metilpiridin-3-il)-1,3,4-tiadiazol-2-il)nicotinamida, ni N-metil-N-(5-(6-metilpiridin-3-il)-1,3,4-tiadiazol-2-il)isonicotinamida.
ARP090103915A 2008-10-14 2009-10-13 Derivados de 2-amidotiadiazol, agonistas de los receptores s1p1 AR073821A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08382042A EP2177521A1 (en) 2008-10-14 2008-10-14 New 2-Amidothiadiazole Derivatives

Publications (1)

Publication Number Publication Date
AR073821A1 true AR073821A1 (es) 2010-12-01

Family

ID=40386238

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090103915A AR073821A1 (es) 2008-10-14 2009-10-13 Derivados de 2-amidotiadiazol, agonistas de los receptores s1p1

Country Status (20)

Country Link
US (1) US20110200557A1 (es)
EP (2) EP2177521A1 (es)
JP (1) JP2012505260A (es)
KR (1) KR20110067034A (es)
CN (1) CN102186847A (es)
AR (1) AR073821A1 (es)
AU (1) AU2009304274A1 (es)
BR (1) BRPI0914371A2 (es)
CA (1) CA2740614A1 (es)
CL (1) CL2011000795A1 (es)
CO (1) CO6321168A2 (es)
EA (1) EA201100612A1 (es)
EC (1) ECSP11010842A (es)
IL (1) IL211290A0 (es)
MX (1) MX2011003692A (es)
PE (1) PE20110420A1 (es)
TW (1) TW201018679A (es)
UY (1) UY32167A (es)
WO (1) WO2010043377A1 (es)
ZA (1) ZA201101236B (es)

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Also Published As

Publication number Publication date
MX2011003692A (es) 2011-04-27
EP2334670A1 (en) 2011-06-22
EP2177521A1 (en) 2010-04-21
AU2009304274A1 (en) 2010-04-22
US20110200557A1 (en) 2011-08-18
WO2010043377A1 (en) 2010-04-22
UY32167A (es) 2010-01-05
ECSP11010842A (es) 2011-03-31
IL211290A0 (en) 2011-04-28
PE20110420A1 (es) 2011-07-01
CA2740614A1 (en) 2010-04-22
KR20110067034A (ko) 2011-06-20
CN102186847A (zh) 2011-09-14
BRPI0914371A2 (pt) 2019-09-24
TW201018679A (en) 2010-05-16
ZA201101236B (en) 2011-09-28
CO6321168A2 (es) 2011-09-20
CL2011000795A1 (es) 2011-08-19
EA201100612A1 (ru) 2011-12-30
JP2012505260A (ja) 2012-03-01

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