AR099160A1 - Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de trastornos inflamatorios - Google Patents

Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de trastornos inflamatorios

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Publication number
AR099160A1
AR099160A1 ARP150100176A ARP150100176A AR099160A1 AR 099160 A1 AR099160 A1 AR 099160A1 AR P150100176 A ARP150100176 A AR P150100176A AR P150100176 A ARP150100176 A AR P150100176A AR 099160 A1 AR099160 A1 AR 099160A1
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AR
Argentina
Prior art keywords
halo
independently selected
alkyl
optionally substituted
diseases
Prior art date
Application number
ARP150100176A
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English (en)
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Galapagos Nv
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Publication of AR099160A1 publication Critical patent/AR099160A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (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)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se revelan bencimidazoles, capaces de inhibir la JAK, estos compuestos se pueden preparar como una composición farmacéutica, y se pueden utilizar para la prevención y el tratamiento de una variedad de afecciones en mamíferos que incluyen seres humanos, que incluyen a modo de ejemplo no limitativo, enfermedades alérgicas, enfermedades inflamatorias, enfermedades autoinmunes, enfermedades proliferativas, rechazo de trasplantes, enfermedades que implican un deterioro del recambio de los cartílagos, malformaciones congénitas de los cartílagos, y/o enfermedades asociadas con la hipersecreción de IL6 o la hipersecreción de interferones. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1) donde R¹ es H o Me; L¹ es -NR²-; -O-, o -CH₂-; Cy es fenilo, o un heteroarilo monocíclico de 5 a 9 miembros o bicíclico condensado que comprende de 1 a 4 heteroátomos seleccionados en forma independiente entre N, O, y S; R² es H, o alquilo C₁₋₄; R³ es H, halo, alquilo C₁₋₄ sustituido en forma opcional con uno o más halo, o alcoxi C₁₋₄ sustituido en forma opcional con uno o más halo; R⁴ es H, o halo; R⁵ es -CN, halo, o es -L²-R⁶; -L² está ausente, o es -C(=O)-, -C(=O)NR⁷-, -NR⁷C(=O)-, -SO₂-, -SO₂NR⁷-, o -NR⁷SO₂-; R⁶ es H, o alquilo C₁₋₆ sustituido en forma opcional con uno o más grupos R⁸ seleccionados en forma independiente; R⁷ es H, o alquilo C₁₋₄; R⁸ es OH, CN, halo, o alcoxi C₁₋₄; Lᵃ está ausente, o es -C(=O)-, -C(=O)O-, o -C(=O)NH-; Rᵃ es: H, alquilo C₁₋₄ sustituido en forma opcional con uno o mas Rᵇ seleccionados en forma independiente, cicloalquilo C₃₋₇ monocíclico sustituido en forma opcional con uno o más Rᶜ seleccionados en forma independiente, o heterocicloalquilo monocíclico de 4 a 7 miembros que comprende uno o más heteroátomos seleccionados en forma independiente de O, N, y S, o heteroarilo monocíclico de 5 a 6 miembros que comprende uno o más heteroátomos seleccionados en forma independiente de O, N y S; Rᵇ es halo, CN, OH, alcoxi C₁₋₄, cicloalquilo C₃₋₇, heterocicloalquilo monocíclico de 4 a 7 miembros que comprende uno o más heteroátomos seleccionados en forma independiente de O, N, y S (dicho heterocicloalquilo está sustituido en forma opcional con uno o más halo u oxo seleccionados en forma independiente), alquilo -SO₂-C₁₋₄, o -C(=O)NRᵇ¹Rᵇ²; Rᶜ es halo, CN, OH, alquilo C₁₋₄, -C(=O)OH, o -C(=O)NRᶜ¹Rᶜ²; y cada Rᵇ¹, Rᵇ², Rᶜ¹ y Rᶜ² se selecciona en forma independiente entre H y alquilo C₁₋₄; o una sal aceptable para uso farmacéutico, o un solvato, o un solvato de la sal aceptable para uso farmacéutico.
ARP150100176A 2014-01-23 2015-01-22 Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de trastornos inflamatorios AR099160A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB1401086.2A GB201401086D0 (en) 2014-01-23 2014-01-23 Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Publications (1)

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AR099160A1 true AR099160A1 (es) 2016-07-06

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ID=50287405

Family Applications (1)

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ARP150100176A AR099160A1 (es) 2014-01-23 2015-01-22 Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de trastornos inflamatorios

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US (3) US9440929B2 (es)
EP (2) EP3097083B1 (es)
JP (1) JP6472454B2 (es)
CN (1) CN106132934B (es)
AR (1) AR099160A1 (es)
AU (1) AU2015208269B2 (es)
BR (1) BR112016016732B1 (es)
CA (1) CA2941474A1 (es)
CY (1) CY1120679T1 (es)
DK (1) DK3097083T3 (es)
EA (1) EA029827B1 (es)
ES (1) ES2693019T3 (es)
GB (1) GB201401086D0 (es)
HR (1) HRP20181332T1 (es)
HU (1) HUE039450T2 (es)
IL (1) IL246823B (es)
LT (1) LT3097083T (es)
MX (1) MX370546B (es)
MY (1) MY180363A (es)
NZ (1) NZ723313A (es)
PH (1) PH12016501677B1 (es)
PL (1) PL3097083T3 (es)
PT (1) PT3097083T (es)
SG (1) SG11201606971XA (es)
SI (1) SI3097083T1 (es)
TW (1) TWI689496B (es)
WO (1) WO2015110378A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR105400A1 (es) 2015-08-04 2017-09-27 Lilly Co Eli Inhibidores de jak1
SI3484875T1 (sl) * 2016-07-14 2021-08-31 Eli Lilly And Company Derivati pirazolilaminobenzimidazola kot zaviralci JAK
GB201717260D0 (en) * 2017-10-20 2017-12-06 Galapagos Nv Novel compounds and pharma ceutical compositions thereof for the treatment of inflammatory disorders
CN108355618B (zh) * 2018-02-27 2020-09-08 江南大学 牛来源透明质酸酶亲和介质及其吸附方法
CN108776121B (zh) * 2018-04-08 2021-07-30 广州卡马生物科技有限公司 一种基于荧光猝灭原理对药材中抗氧剂的高通量筛选方法
MX2021003093A (es) * 2018-09-18 2021-05-12 Terns Inc Compuestos para tratar ciertas leucemias.
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
GB201904373D0 (en) * 2019-03-29 2019-05-15 Galapagos Nv Novel compounds and pharamaceutical compositions thereof for the treatment of inflammatory disorders
CN114671858B (zh) * 2022-03-07 2023-08-08 华中师范大学 一种苯并咪唑系化合物及其制备方法与应用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070004658A1 (en) 2004-06-21 2007-01-04 Nick Vandeghinste Method and means for treatment of osteoarthritis
US20100311965A1 (en) * 2007-12-28 2010-12-09 Carna Biosciences Inc. 2-aminoquinazoline derivative
BRPI0910668A2 (pt) * 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
WO2012044090A2 (ko) * 2010-09-29 2012-04-05 크리스탈지노믹스(주) 단백질 키나제 억제 활성을 갖는 신규한 아미노퀴나졸린 화합물
UY34616A (es) * 2012-02-10 2013-09-30 Galapagos Nv Nuevo compuesto útil para el tratamiento de enfermedades degenerativas e inflamatorias.

Also Published As

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EP3395802A1 (en) 2018-10-31
US20190152922A1 (en) 2019-05-23
AU2015208269A1 (en) 2016-09-01
BR112016016732B1 (pt) 2023-04-18
HRP20181332T1 (hr) 2018-10-19
ES2693019T3 (es) 2018-12-07
WO2015110378A1 (en) 2015-07-30
HUE039450T2 (hu) 2018-12-28
US10179771B2 (en) 2019-01-15
SI3097083T1 (sl) 2018-10-30
AU2015208269B2 (en) 2018-08-30
TW201613873A (en) 2016-04-16
US9440929B2 (en) 2016-09-13
PH12016501677A1 (en) 2016-11-07
EP3097083A1 (en) 2016-11-30
JP2017503834A (ja) 2017-02-02
CY1120679T1 (el) 2019-12-11
SG11201606971XA (en) 2016-10-28
GB201401086D0 (en) 2014-03-12
MX2016009442A (es) 2016-10-13
EP3097083B1 (en) 2018-08-08
EA029827B1 (ru) 2018-05-31
CA2941474A1 (en) 2015-07-30
DK3097083T3 (en) 2018-10-01
BR112016016732A8 (pt) 2020-06-16
NZ723313A (en) 2019-11-29
TWI689496B (zh) 2020-04-01
IL246823B (en) 2020-02-27
LT3097083T (lt) 2018-11-26
IL246823A0 (en) 2016-08-31
CN106132934A (zh) 2016-11-16
PH12016501677B1 (en) 2016-11-07
PT3097083T (pt) 2018-10-26
US20150203455A1 (en) 2015-07-23
MY180363A (en) 2020-11-28
CN106132934B (zh) 2019-04-02
JP6472454B2 (ja) 2019-02-20
EA201691468A1 (ru) 2016-12-30
US20170057928A1 (en) 2017-03-02
PL3097083T3 (pl) 2018-11-30
MX370546B (es) 2019-12-17

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