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AR082974A1 - Derivados de azabenzotiazol, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos para tratar enfermedades inflamatorias - Google Patents

Derivados de azabenzotiazol, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos para tratar enfermedades inflamatorias

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Publication number
AR082974A1
AR082974A1 ARP110103333A ARP110103333A AR082974A1 AR 082974 A1 AR082974 A1 AR 082974A1 AR P110103333 A ARP110103333 A AR P110103333A AR P110103333 A ARP110103333 A AR P110103333A AR 082974 A1 AR082974 A1 AR 082974A1
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AR
Argentina
Prior art keywords
alkylene
halogen
alkyl
optionally substituted
oxo
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Application number
ARP110103333A
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English (en)
Inventor
Simon Goodacre
Yingjie Lai
Jun Liang
Calum Macleod
Karen Williams
Birong Zhang
Vickie Tsui
Toby Blench
Charles Ellwood
Steven Magnuson
Original Assignee
Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR082974A1 publication Critical patent/AR082974A1/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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • 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
    • 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
    • A61P37/08—Antiallergic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) estereoisómeros, tautómeros, solvatos, profármacos y sales farmacéuticamente aceptables del mismo, en la que A es CR3 o N; X es CR15 o N; R1 es con independencia hidrógeno, halógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, -CF3, -OR6, -SR6, -OCF3, -CN, -NO2, -C(O)R6, -C(O)OR6, -C(O)NR6R7, -S(O)1-2R6, -S(O)1-2NR6R7, -NR6S(O)1-2R7, -NR6SO2NR6R7, -NR6C(O)R7, -NR6C(O)OR7, -NR6C(O)NR6R7, -OC(O)NR6R7 o -NR6R7, en la que los dos R1 no pueden ser hidrógeno al mismo tiempo y dichos alquilo, alquenilo, alquinilo y cicloalquilo están opcionalmente sustituidos por halógeno, oxo, -CN, OR6, -NR6R7, cicloalquilo C3-6, heterociclilo de 3 - 6 eslabones o fenilo y dichos cicloalquilo, heterociclilo y fenilo están opcionalmente sustituidos con independencia por R10; R2 y R3 son en cada caso con independencia hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halógeno, -(alquileno C0-3)CN, -(alquileno C0-3)OR8, -(alquileno C0-3)SR8, -(alquileno C0-3)NR8R9, -(alquileno C0-3)CF3, -O(alquileno C0-3)CF3, -(alquileno C0-3)NO2, -(alquileno C0-3)C(O)R8, -(alquileno C0-3)C(O)OR8, -(alquileno C0-3)C(O)NR8R9, -(alquileno C0-3)NR8C(O)R9, -(alquileno C0-3)S(O)1-2R8, -(alquileno C0-3)NR8S(O)1-2R9, -(alquileno C0-3)S(O)1-2NR8R9, -(alquileno C0-3)(cicloalquilo C3-6), -(alquileno C0-3)(heterociclilo de 3 - 10 eslabones), -(alquileno C0-3)(heteroarilo de 5 - 10 eslabones) o -(alquileno C0-3)fenilo, dichos R2 y R3 están en cada caso opcionalmente sustituidos con independencia por R10; R4 es hidrógeno, -NR6-, -NR6R7, -NR6C(O)-, -NR6C(O)O-, -NR6C(O)NR7-, -NR6S(O)1-2- o -NR6S(O)1-2NR7-; R5 está ausente, o es hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-10, heterociclilo de 3 - 10 eslabones o heteroarilo de 5 - 10 eslabones, dicho R5 está opcionalmente sustituido por R10; R6 y R7 son en cada caso con independencia hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6 o cicloalquilo C3-6, dichos alquilo, alquenilo, alquinilo y cicloalquilo están opcionalmente sustituidos con independencia por halógeno, alquilo C1-6, oxo; -CN, -OR11 o -NR11R12; o R6 y R7 junto con el átomo al que están unidos forman con independencia un heterociclilo de 3 - 6 eslabones opcionalmente sustituido por halógeno, oxo, -OR11, -NR11R12 o alquilo C1-6 opcionalmente sustituido por halógeno; R8 y R9 son en cada caso con independencia hidrógeno, alquilo C1-6, cicloalquilo C3-6, fenilo, heterociclilo de 3 - 6 eslabones o heteroarilo de 5 - 6 eslabones, dichos alquilo, cicloalquilo, fenilo, heterociclilo o heteroarilo están opcionalmente sustituidos con independencia por R10; o R8 y R9 junto con el átomo al que están unidos forman con independencia un heterociclilo de 3 - 6 eslabones opcionalmente sustituido por halógeno, oxo, -NR11R12 o alquilo C1-6; R10 es con independencia hidrógeno, oxo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halógeno, -(alquileno C0-3)CN, -(alquileno C0-3)OR11, -(alquileno C0-3)SR11, -(alquileno C0-3)NR11R12, -(alquileno C0-3)CF3, -(alquileno C0-3)NO2, -C=NH(OR11), -(alquileno C0-3)C(O)R11, -(alquileno C0-3)C(O)OR11, -(alquileno C0-3)C(O)NR11R12, -(alquileno C0-3)NR11C(O)R12, -(alquileno C0-3)S(O)1-2R11, -(alquileno C0-3)NR11S(O)1-2R12, -(alquileno C0-3)S(O)1-2NR11R12, -(alquileno C0-3)(cicloalquilo C3-6), -(alquileno C0-3)(heterociclilo de 3 - 10 eslabones), -(alquileno C0-3)C(O)(heterociclilo de 3 - 10 eslabones), -(alquileno C0-3)(heteroarilo de 5 - 10 eslabones) o -(alquileno C0-3)fenilo, dicho R10 está opcionalmente sustituido con independencia por halógeno, oxo, -CF3, -(alquileno C0-3)OR13, -(alquileno C0-3)NR13R14, -(alquileno C0-3)C(O)R13, -(alquileno C0-3)S(O)1-2R13 o alquilo C1-6 opcionalmente sustituido por oxo, -CN o halógeno; R11 y R12 son en cada caso con independencia hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, fenilo, heteroarilo de 5 - 6 eslabones o heterociclilo de 3 - 6 eslabones, dichos alquilo, alquenilo, alquinilo, cicloalquilo, fenilo, heteroarilo y heterociclilo están opcionalmente sustituidos con independencia por halógeno, oxo, -CN, -OR16, -NR16R17 o alquilo C1-6 opcionalmente sustituido por halógeno, -CN u oxo; o R11 y R12 junto con el átomo al que están unidos forman un heterociclilo de 3 - 6 eslabones opcionalmente sustituido por halógeno, oxo, -OR16, -NR16R17 o alquilo C1-6 opcionalmente sustituido por halógeno, oxo u OH; R13 y R14 son en cada caso con independencia hidrógeno o alquilo C1-6 opcionalmente sustituido por halógeno u oxo; o R13 y R14 junto con el átomo al que están unidos forman un heterociclilo de 3 - 6 eslabones opcionalmente sustituido por halógeno, oxo o alquilo C1-6 opcionalmente sustituido por halógeno u oxo; R15 es hidrógeno, halógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -(alquileno C0-3)CN, -(alquileno C0-3)OR18, -(alquileno C0-3)SR18, -(alquileno C0-3)NR18R19, -(alquileno C0-3)CF3, -O(alquileno C0-3)CF3, -(alquileno C0-3)NO2, -(alquileno C0-3)C(O)R18, -(alquileno C0-3)C(O)OR18, -(alquileno C0-3)C(O)NR18R19, -(alquileno C0-3)NR18C(O)R19, -(alquileno C0-3)S(O)1-2R18, -(alquileno C0-3)NR18S(O)1-2R19, -(alquileno C0-3)-S(O)1-2NR18R19, -(alquileno C0-3)(cicloalquilo C3-6), -(alquileno C0-3)(heterociclilo de 3 - 6 eslabones), -(alquileno C0-3)(heteroarilo de 5 - 6 eslabones) o -(alquileno C0-3)fenilo; R16 y R17 son en cada caso con independencia hidrógeno o alquilo C1-6 opcionalmente sustituido por halógeno u oxo; o R16 y R17 junto con el átomo al que están unidos forman un heterociclilo de 3 - 6 eslabones opcionalmente sustituido por halógeno, oxo o alquilo C1-6 opcionalmente sustituido por oxo o halógeno; y R18 y R19 son en cada caso con independencia hidrógeno o alquilo C1-6 opcionalmente sustituido por halógeno u oxo; que son distintos de la 2-(2-clorofenil)tiazolo[5,4-c]-piridina, 2-(tiazolo[5,4-c]piridin-2-il)anilina, 2-fenoxi-N-(2-tiazolo[5,4-c]piridin-2-il-fenil)-propanamida, N-(2-tiazolo[5,4-c]piridin-2-il-fenil)-bencenopropanamida, 2-(2-metilfenil)-tiazolo[5,4-c]piridina, 2-[2-metoxi-4-(metiltio)-fenil]-tiazolo[5,4-c]piridina y 2-(2,6-diclorofenil)tiazolo-[5,4-c]piridina.
ARP110103333A 2010-09-15 2011-09-14 Derivados de azabenzotiazol, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos para tratar enfermedades inflamatorias AR082974A1 (es)

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