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AR101395A1 - Derivados de indolizina y su uso en enfermedades neurodegenerativas - Google Patents

Derivados de indolizina y su uso en enfermedades neurodegenerativas

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Publication number
AR101395A1
AR101395A1 ARP150102464A ARP150102464A AR101395A1 AR 101395 A1 AR101395 A1 AR 101395A1 AR P150102464 A ARP150102464 A AR P150102464A AR P150102464 A ARP150102464 A AR P150102464A AR 101395 A1 AR101395 A1 AR 101395A1
Authority
AR
Argentina
Prior art keywords
sulfur
nitrogen
oxygen
ring
nrc
Prior art date
Application number
ARP150102464A
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English (en)
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Merck Patent Gmbh
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Publication date
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Publication of AR101395A1 publication Critical patent/AR101395A1/es

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    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
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    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P37/08Antiallergic agents
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Nutrition Science (AREA)
  • Otolaryngology (AREA)
  • Anesthesiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde: X es -halógeno, -haloalquilo, -O, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, -NRC(O)N(R)₂, -NRSO₂R o -N(R)₂; o X es un alifático C₁₋₆, arilo C₅₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre, o un anillo heteroarílico monocíclico de 5 a 6 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre; estando cada uno de los cuales opcionalmente sustituido; Y es O, S, SO₂, SO, C(O), CO₂, C(O)N(R), NRC(O), NRC(O)N(R), NRSO₂ o N(R); el anillo A es arilo C₅₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre, o un anillo heteroarílico monocíclico de 5 a 6 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre; o un anillo bicíclico, bicíclico condensado, espirobicíclico o policíclico de 6 a 18 miembros que tiene de 0 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre, estando cada uno de los cuales opcionalmente sustituido; cada R¹ es, independientemente, -R, halógeno, -haloalquilo, -hidroxialquilo, -O, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, -NRC(O)N(R)₂, -NRSO₂R o -N(R)₂; o dos grupos R¹, junto con el átomo o los átomos a los que cada uno está unido, pueden formar un anillo condensado o espiro seleccionado entre arilo C₅₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre, o un anillo heteroarílico monocíclico de 5 a 6 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre; estando cada uno de los cuales opcionalmente sustituido; Z es -R, halógeno, -haloalquilo, -hidroxialquilo, -O, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, -NRC(O)N(R)₂, -NRSO₂R o -N(R)₂-; cada Rᵃ es, independientemente, -R, halógeno, -haloalquilo, -hidroxialquilo, -O, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, -NRC(O)N(R)₂, -NRSO₂R o -N(R)₂; cada R es, independientemente, hidrógeno, alifático C₁₋₆, arilo C₃₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre, o un anillo heteroarílico monocíclico de 5 a 6 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre; estando cada uno de los cuales opcionalmente sustituido; o dos grupos R del mismo átomo se toman junto con el átomo al que están unidos para formar un arilo C₃₋₁₀, un anillo carbocíclico saturado o parcialmente insaturado de 3 a 8 miembros, un anillo heterocíclico de 3 a 7 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre o un anillo heteroarílico monocíclico de 5 a 6 miembros que tiene de 1 a 4 heteroátomos seleccionados, independientemente, entre nitrógeno, oxígeno o azufre; estando cada uno de los cuales opcionalmente sustituido; m es 1 ó 2; n es 0, 1, 2 ó 3; y p es 0, 1 ó 2.
ARP150102464A 2014-07-31 2015-07-31 Derivados de indolizina y su uso en enfermedades neurodegenerativas AR101395A1 (es)

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US201462031237P 2014-07-31 2014-07-31

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AR101395A1 true AR101395A1 (es) 2016-12-14

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US (2) US9546166B2 (es)
EP (1) EP3174877B1 (es)
JP (1) JP6571756B2 (es)
KR (1) KR20170033339A (es)
CN (1) CN107001356B (es)
AR (1) AR101395A1 (es)
AU (1) AU2015296210B2 (es)
BR (1) BR112017001221A2 (es)
CA (1) CA2954681A1 (es)
ES (1) ES2927587T3 (es)
IL (1) IL250267B (es)
MX (1) MX2017001103A (es)
RU (1) RU2017105133A (es)
SG (1) SG11201700140TA (es)
WO (1) WO2016019228A1 (es)

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DE102010030111A1 (de) 2009-08-11 2011-02-17 Evonik Degussa Gmbh Wässrige Silansysteme für den Blankkorrosionsschutz und Korrosionsschutz von Metallen
CN107709299B (zh) 2015-04-24 2021-07-16 盐野义制药株式会社 6元杂环衍生物及含有其的药物组合物
CN116332886A (zh) 2016-07-18 2023-06-27 广州瑞安博医药科技有限公司 用于治疗或预防与痛风或高尿酸血症相关的症状的化合物、组合物和方法
RU2753524C2 (ru) 2016-10-17 2021-08-17 Сионоги Энд Ко., Лтд. Бициклические азотсодержащие гетероциклические производные и включающие их фармацевтические композиции
FI3609868T3 (fi) 2017-03-13 2023-11-22 Raqualia Pharma Inc Tetrahydrokinoliinijohdannaisia P2X7-reseptorin antagonisteina
CA3088968C (en) * 2018-01-18 2023-10-17 Daiichi Sankyo Company, Limited Dihydroindolizinone derivative
EA202191545A1 (ru) 2018-12-06 2021-10-28 Артроси Терапьютикс, Инк. Кристаллические формы соединения для лечения или профилактики подагры или гиперурикемии
EP3890722A4 (en) 2018-12-06 2022-08-24 Arthrosi Therapeutics, Inc. METHODS OF TREATMENT OR PREVENTION OF GOUT OR HYPERURICEMIA
AU2020256166A1 (en) 2019-04-02 2021-10-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5
JP7553030B2 (ja) * 2019-07-08 2024-09-18 国立大学法人東京工業大学 ジヒドロインドリジノン誘導体を用いたインスリン産生細胞の作製法

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DE19731153A1 (de) * 1997-07-21 1999-01-28 Basf Ag 2-(Pyrazolyl- und Triazolyl-3'-oxymethylen)-phenyl-isoxazolone und -triazolone, Verfahren zu ihrer Herstellung und ihre Verwendung
AU2001278006A1 (en) 2000-07-27 2002-02-13 Smithkline Beecham Corporation Agonists of follicle stimulating hormone activity
CN101848909A (zh) * 2006-02-14 2010-09-29 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡咯并[3,2-c]吡啶
WO2008124153A1 (en) * 2007-04-10 2008-10-16 H. Lundbeck A/S Heteroaryl amide analogues as p2x7 antagonists
DK2835131T3 (en) * 2010-12-14 2017-12-04 Electrophoretics Ltd Casein kinase 1 delta inhibitors (CK1 delta)

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ES2927587T3 (es) 2022-11-08
EP3174877A1 (en) 2017-06-07
US20160031879A1 (en) 2016-02-04
WO2016019228A1 (en) 2016-02-04
US9546166B2 (en) 2017-01-17
EP3174877B1 (en) 2022-06-29
IL250267B (en) 2021-05-31
JP2017522347A (ja) 2017-08-10
CA2954681A1 (en) 2016-02-04
MX2017001103A (es) 2017-04-27
BR112017001221A2 (pt) 2017-11-28
AU2015296210B2 (en) 2019-08-15
SG11201700140TA (en) 2017-02-27
CN107001356B (zh) 2019-09-03
IL250267A0 (en) 2017-03-30
US9931324B2 (en) 2018-04-03
CN107001356A (zh) 2017-08-01
JP6571756B2 (ja) 2019-09-04
KR20170033339A (ko) 2017-03-24
AU2015296210A1 (en) 2017-02-02
RU2017105133A (ru) 2018-08-28
US20170079965A1 (en) 2017-03-23

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