EA025086B9 - Производные индоламида и родственные соединения для использования при лечении нейродегенеративных заболеваний - Google Patents

Производные индоламида и родственные соединения для использования при лечении нейродегенеративных заболеваний

Info

Publication number
EA025086B9
EA025086B9 EA201200002A EA201200002A EA025086B9 EA 025086 B9 EA025086 B9 EA 025086B9 EA 201200002 A EA201200002 A EA 201200002A EA 201200002 A EA201200002 A EA 201200002A EA 025086 B9 EA025086 B9 EA 025086B9
Authority
EA
Eurasian Patent Office
Prior art keywords
novel compounds
treatment
disorders
neurodegenerative diseases
related compounds
Prior art date
Application number
EA201200002A
Other languages
English (en)
Other versions
EA201200002A1 (ru
EA025086B1 (ru
Inventor
Герард Гриффиун
Дорен Том Ван
Де Ла Парра Вероника Ройас
Арно Маршан
Сара Алласиа
Амюри Килонда
Патрик Шалтен
Original Assignee
Католике Университейт Лёвен, К.У. Лёвен Р Энд Д
Реминд
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 Католике Университейт Лёвен, К.У. Лёвен Р Энд Д, Реминд filed Critical Католике Университейт Лёвен, К.У. Лёвен Р Энд Д
Publication of EA201200002A1 publication Critical patent/EA201200002A1/ru
Publication of EA025086B1 publication Critical patent/EA025086B1/ru
Publication of EA025086B9 publication Critical patent/EA025086B9/ru

Links

Classifications

    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41921,2,3-Triazoles
    • 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

В данном изобретении предлагаются новые соединения формулы (АА1), а также соединения для применения в качестве лекарственного средства для профилактики или лечения нейродегенеративного расстройства, более конкретно некоторых неврологических расстройств, таких как расстройства, совокупно известные как таупатии, и расстройства, характеризующиеся амилоидогенезом цитотоксического α-синуклеина. Данное изобретение также относится к применению указанных новых соединений для производства лекарственных средств, пригодных для лечения таких нейродегенеративных расстройств. Данное изобретение дополнительно относится к фармацевтическим композициям, в том числе содержащим указанные новые соединения, и способам получения указанных новых соединений
EA201200002A 2009-06-11 2010-06-11 Производные индоламида и родственные соединения для использования при лечении нейродегенеративных заболеваний EA025086B9 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0910003.3A GB0910003D0 (en) 2009-06-11 2009-06-11 Novel compounds for the treatment of neurodegenerative diseases
PCT/EP2010/058271 WO2010142801A1 (en) 2009-06-11 2010-06-11 Indole amide derivatives and related compounds for use in the treatment of neurodegenerative diseases

Publications (3)

Publication Number Publication Date
EA201200002A1 EA201200002A1 (ru) 2012-05-30
EA025086B1 EA025086B1 (ru) 2016-11-30
EA025086B9 true EA025086B9 (ru) 2017-01-30

Family

ID=40937200

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201200002A EA025086B9 (ru) 2009-06-11 2010-06-11 Производные индоламида и родственные соединения для использования при лечении нейродегенеративных заболеваний

Country Status (13)

Country Link
US (4) US8618138B2 (ru)
EP (2) EP3190109B1 (ru)
JP (1) JP6116245B2 (ru)
CN (1) CN102803252B (ru)
AU (1) AU2010258566B2 (ru)
CA (1) CA2765181C (ru)
EA (1) EA025086B9 (ru)
ES (1) ES2627957T3 (ru)
GB (1) GB0910003D0 (ru)
HR (1) HRP20170731T1 (ru)
HU (1) HUE034733T2 (ru)
SI (1) SI2440550T1 (ru)
WO (1) WO2010142801A1 (ru)

Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
WO2011047156A1 (en) * 2009-10-15 2011-04-21 Hercules Technology Management Co V, Inc. Sepiapterin reductase inhibitors for the treatment of pain
KR20120112548A (ko) * 2009-12-16 2012-10-11 뉴로포레 테라피스, 인코포레이티드 시누클레인 병을 치료하는데 적합한 화합물
GB201021103D0 (en) * 2010-12-13 2011-01-26 Univ Leuven Kath New compounds for the treatment of neurodegenerative diseases
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
AR086113A1 (es) 2011-04-30 2013-11-20 Abbott Lab Isoxazolinas como agentes terapeuticos
GB201116559D0 (en) 2011-09-26 2011-11-09 Univ Leuven Kath Novel viral replication inhibitors
EP2807157A1 (en) * 2012-01-27 2014-12-03 Novartis AG 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
SG10201507714XA (en) 2012-03-16 2015-10-29 Axikin Pharmaceuticals Inc 3,5-diaminopyrazole kinase inhibitors
EP2666766A1 (en) 2012-05-21 2013-11-27 Dr. August Wolff GmbH & Co. KG Arzneimittel Novel E,E-diene compounds and their use as medicaments and cosmetics
ME02651B (me) 2012-06-13 2017-06-20 Incyte Holdings Corp Substituisana triciklična jedinjenja kao inhibitori fgfr
CA2877983A1 (en) 2012-07-16 2014-01-23 Neuropore Therapies, Inc. Di- and tri-heteroaryl derivatives as inhibitors of protein aggregation
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EP2952096B1 (en) * 2013-01-30 2018-04-04 Sumitomo Chemical Company, Limited Amide compound, an arthropod pest control agent and a method for controlling arthropod pest
CA2909207C (en) 2013-04-19 2021-11-02 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
RU2712621C2 (ru) 2013-05-23 2020-01-30 Калвиста Фармасьютикалз Лимитед Азотсодержащие гетероциклические производные, полезные в качестве ингибитора калликреина плазмы
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
CN105683179B (zh) 2013-08-14 2018-10-26 卡尔维斯塔制药有限公司 血浆激肽释放酶的抑制剂
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
NZ631142A (en) 2013-09-18 2016-03-31 Axikin Pharmaceuticals Inc Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors
RS57533B1 (sr) * 2014-01-29 2018-10-31 Ucb Biopharma Sprl Heteroaril amidi kao inhibitori proteinske agregacije
EP3110794A1 (en) * 2014-02-27 2017-01-04 Merck Patent GmbH Heterocyclic compounds as nav channel inhibitors and uses thereof
AU2015229188A1 (en) 2014-03-13 2016-09-29 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing CFTR activity
WO2015138934A1 (en) 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
US10149836B2 (en) 2014-03-21 2018-12-11 The Board Of Regents Of The University Of Texas System Isoxazole treatments for frontotemporal dementia
WO2015196071A1 (en) 2014-06-19 2015-12-23 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr activity
MA40759A (fr) 2014-09-26 2017-08-01 Pfizer Modulateurs de rorc2 de type pyrrolopyridine substitué par un méthyle et trifluorométhyle et leurs procédés d'utilisation
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
CN107250116B (zh) 2014-12-23 2020-10-27 艾士盟医疗公司 3,5-二氨基吡唑激酶抑制剂
MA41253A (fr) * 2014-12-23 2017-10-31 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
WO2016105468A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis
US10392378B2 (en) 2014-12-23 2019-08-27 Proteostasis Therapeutics, Inc. Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis
WO2016105484A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
JOP20160086B1 (ar) 2015-05-08 2021-08-17 2 Katholieke Univ Leuven Ku Leuven Research And Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
RS59934B1 (sr) 2015-06-09 2020-03-31 Abbvie Inc Modulatori nuklearnih receptora (ror) za lečenje inflamatornih i autoimunih oboljenja
AU2016297886B2 (en) 2015-07-24 2020-12-10 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing CFTR activity
US10975066B2 (en) 2015-07-29 2021-04-13 UCB Biopharma SRL Bis-heteroaryl derivatives as modulators of protein aggregation
JO3633B1 (ar) * 2015-09-16 2020-08-27 Katholieke Univ Leuven Ku Leuven Research & Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JOP20160198B1 (ar) 2015-09-16 2022-03-14 Janssen Pharmaceuticals Inc مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
EP3359536B1 (en) 2015-10-06 2021-08-04 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for modulating cftr
EP3436435B1 (en) 2016-03-31 2021-05-12 Janssen Pharmaceuticals, Inc. Substituted indole derivatives as dengue viral replication inhibitors
SG11201808270PA (en) 2016-03-31 2018-10-30 Janssen Pharmaceuticals Inc Substituted indoline derivatives as dengue viral replication inhibitors
MA44502A (fr) 2016-04-01 2019-02-06 Janssen Pharmaceuticals Inc Dérivés d'indole substitués utilisés en tant qu'inhibiteurs de réplication du virus de la dengue
JOP20170069B1 (ar) 2016-04-01 2021-08-17 1 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
AR108203A1 (es) 2016-04-07 2018-07-25 Proteostasis Therapeutics Inc Compuestos, composiciones y métodos para modular cftr (regulador de la conductancia transmembrana de la fibrosis quística)
KR20220107319A (ko) 2016-05-31 2022-08-02 칼비스타 파마슈티컬즈 리미티드 혈장 칼리크레인 저해제로서 피라졸 유도체
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
US10899751B2 (en) 2016-06-21 2021-01-26 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing CFTR activity
RU2019126170A (ru) 2017-01-26 2021-02-26 Юсб Байофарма Спрл Бисгетероарильные производные в качестве модуляторов агрегации белков
MX2019007054A (es) 2017-01-26 2019-08-29 Ucb Biopharma Sprl Derivados de alcoxi bis-heteroarilo como moduladores de la agregacion de proteinas.
EA201991755A1 (ru) 2017-01-26 2020-01-22 Юсб Байофарма Спрл Бициклические бисгетероарильные производные в качестве модуляторов агрегации белков
JOP20180026A1 (ar) 2017-03-31 2019-01-30 Univ Leuven Kath مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JOP20180025B1 (ar) 2017-03-31 2021-08-17 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
EP3395803A1 (en) 2017-04-28 2018-10-31 Institut Pasteur Imidazopyrazine derivatives, process for preparation thereof, and their uses as luciferins
EP3634407A1 (en) 2017-05-11 2020-04-15 Remynd N.V. Inhibitors of pde6delta for use in the prevention and/or treatment of epilepsy and/or neurodegenerative disorders
EA201992397A1 (ru) * 2017-05-11 2020-03-16 Реминд Н.В. Соединения для лечения эпилепсии, нейродегенеративных нарушений и других нарушений цнс
KR102625991B1 (ko) 2017-05-22 2024-01-16 얀센 파마슈티칼즈, 인코포레이티드 뎅기 바이러스 복제 억제제로서의 치환 인돌린 유도체
KR102625988B1 (ko) 2017-05-22 2024-01-16 얀센 파마슈티칼즈, 인코포레이티드 뎅기 바이러스 복제 억제제로서의 치환 인돌린 유도체
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JP7169592B2 (ja) 2017-09-27 2022-11-11 国立大学法人 鹿児島大学 Pac1受容体拮抗薬を用いた鎮痛薬
HRP20220367T1 (hr) 2017-11-29 2022-05-27 Kalvista Pharmaceuticals Limited Oblici za doziranje koji sadrže plazmatski kalikrein inhibitor
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
CA3092927A1 (en) 2018-03-05 2019-09-12 Bristol-Myers Squibb Company Phenylpyrrolidinone formyl peptide 2 receptor agonists
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
WO2019213544A2 (en) 2018-05-04 2019-11-07 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
JP2022508648A (ja) 2018-10-05 2022-01-19 アンナプルナ バイオ インコーポレイテッド Apj受容体活性に関連する状態を処置するための化合物および組成物
US11807622B2 (en) 2019-01-30 2023-11-07 Insilico Medicine Ip Limited TLR 9 inhibitors
US10689360B1 (en) * 2019-01-30 2020-06-23 Insilico Medicine Ip Limited TLR inhibitors
JP7501920B2 (ja) 2019-02-27 2024-06-18 国立大学法人 鹿児島大学 Pac1受容体拮抗薬を用いた鎮痒薬
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021023858A1 (en) * 2019-08-08 2021-02-11 Université De Strasbourg TrkB POSITIVE ALLOSTERIC MODULATORS
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CN112480100B (zh) * 2019-09-11 2022-10-14 康威(广州)生物科技有限公司 吡咯烷酮衍生物
EP4025212A4 (en) * 2019-09-27 2023-08-23 Collaborations Pharmaceuticals, Inc. ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASES CAUSED BY VIRUS INFECTION
JOP20220083A1 (ar) 2019-10-14 2023-01-30 Incyte Corp حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021090245A1 (en) 2019-11-06 2021-05-14 Yuhan Corporation Pyrrolidine and piperidine compounds
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
GB2591730A (en) 2019-12-09 2021-08-11 Kalvista Pharmaceuticals Ltd New polymorphs
CA3166986A1 (en) * 2020-01-07 2021-07-15 Sumitomo Pharma Co., Ltd. Therapeutic agent for tauopathies
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11896644B2 (en) * 2020-02-07 2024-02-13 University Of South Florida Inhibition of beta-arrestin oligomerization in tauopathy
EP4147701A4 (en) 2020-05-08 2024-06-12 Kagoshima University ANTIDEPRESSANT/ANXIOLYTIC DRUG WITH PAC1 RECEPTOR ANTAGONIST
WO2022079446A1 (en) 2020-10-15 2022-04-21 Kalvista Pharmaceuticals Limited Treatments of angioedema
EP4232031A1 (en) 2020-10-23 2023-08-30 Kalvista Pharmaceuticals Limited Treatments of angioedema
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
WO2023002219A1 (en) 2021-07-23 2023-01-26 Kalvista Pharmaceuticals Limited Treatments of hereditary angioedema
WO2023209381A1 (en) 2022-04-27 2023-11-02 Kalvista Pharmaceuticals Limited Formulations of a plasma kallikrein inhibitor
CN115974862B (zh) * 2023-01-30 2024-04-19 四川大学华西医院 一种基于protac原理的hl化合物及其制备方法和应用
KR102657677B1 (ko) * 2023-10-26 2024-04-16 국방과학연구소 공융용매 하에서 흐름반응을 이용한 아이소옥사졸의 제조 방법

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0287237A (ja) * 1988-09-22 1990-03-28 Fujitsu Ltd Execute命令制御方式
US5314886A (en) * 1990-12-11 1994-05-24 G. D. Searle & Co. N-substituted lactams useful as cholecystokinin antagonists
WO2000055144A1 (en) * 1999-03-15 2000-09-21 Axys Pharmaceuticals, Inc. Amine derivatives as protease inhibitors
US20050239689A1 (en) * 2001-03-30 2005-10-27 Wisconsin Alumni Research Foundation Vancomycin analogs and methods thereof
WO2005115977A1 (en) * 2004-05-28 2005-12-08 Tanabe Seiyaku Co., Ltd. Pyrrolidine derivatives as cb1-receptor antagonists
US20070105937A1 (en) * 2003-12-22 2007-05-10 Miguel Pappolla Indole-3-propionamide and derivatives thereof

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5416193A (en) * 1993-04-30 1995-05-16 Pfizer Inc. Coupling reagent and method
JPH0987237A (ja) 1995-09-21 1997-03-31 Kyowa Hakko Kogyo Co Ltd 芳香族誘導体
US7101878B1 (en) * 1998-08-20 2006-09-05 Agouron Pharmaceuticals, Inc. Non-peptide GNRH agents, methods and intermediates for their preparation
GB0017676D0 (en) * 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
MXPA06005734A (es) * 2003-11-28 2006-08-17 Hoffmann La Roche Acidos tetronico y tetramico como inhibidores de beta-secretasa.
CN1960970A (zh) * 2004-05-28 2007-05-09 田边制药株式会社 作为cb1受体的拮抗剂的吡咯烷衍生物
RU2007103834A (ru) 2004-07-01 2008-08-10 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния (Us) Ингибирование взаимодействия pdz-доменов малыми молекулами
JP2008007405A (ja) 2004-12-07 2008-01-17 Takeda Chem Ind Ltd カルボキサミド誘導体
US20090105308A1 (en) * 2005-07-12 2009-04-23 Darren Mansfield Benzoheterocylethylcarboxamide derivatives
JP2007194232A (ja) 2006-01-17 2007-08-02 Shin Etsu Handotai Co Ltd シリコン単結晶ウエーハの製造方法
CA2659155A1 (en) * 2006-07-20 2008-01-24 Amgen Inc. Substituted azole aromatic heterocycles as inhibitors of 11.beta.-hsd-1
EP2121621B1 (en) * 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
US20080227823A1 (en) * 2007-03-12 2008-09-18 Hassan Pajouhesh Amide derivatives as calcium channel blockers
EP2002834A1 (de) 2007-06-13 2008-12-17 Bayer Schering Pharma Aktiengesellschaft Aryl/Hetarylamide als Modulatoren des EP2-Rezeptors
US7968536B2 (en) 2007-06-29 2011-06-28 Millennium Pharmaceuticals, Inc. Heterocyclic compounds useful as RAF kinase inhibitors
EP2203427A2 (en) 2007-09-20 2010-07-07 Abbott Healthcare Products B.V. 5-aryl-4,5-dihydro-(1h)-pyrazoles as cannabinoid cb1 receptor agonists
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0287237A (ja) * 1988-09-22 1990-03-28 Fujitsu Ltd Execute命令制御方式
US5314886A (en) * 1990-12-11 1994-05-24 G. D. Searle & Co. N-substituted lactams useful as cholecystokinin antagonists
WO2000055144A1 (en) * 1999-03-15 2000-09-21 Axys Pharmaceuticals, Inc. Amine derivatives as protease inhibitors
US20050239689A1 (en) * 2001-03-30 2005-10-27 Wisconsin Alumni Research Foundation Vancomycin analogs and methods thereof
US20070105937A1 (en) * 2003-12-22 2007-05-10 Miguel Pappolla Indole-3-propionamide and derivatives thereof
WO2005115977A1 (en) * 2004-05-28 2005-12-08 Tanabe Seiyaku Co., Ltd. Pyrrolidine derivatives as cb1-receptor antagonists

Also Published As

Publication number Publication date
CN102803252B (zh) 2016-05-25
EA201200002A1 (ru) 2012-05-30
US10117850B2 (en) 2018-11-06
US9434722B2 (en) 2016-09-06
CN102803252A (zh) 2012-11-28
GB0910003D0 (en) 2009-07-22
US8618138B2 (en) 2013-12-31
WO2010142801A1 (en) 2010-12-16
CA2765181C (en) 2017-04-04
US20190054068A1 (en) 2019-02-21
HUE034733T2 (en) 2018-02-28
JP2012529476A (ja) 2012-11-22
CA2765181A1 (en) 2010-12-16
AU2010258566A1 (en) 2012-01-19
SI2440550T1 (sl) 2017-05-31
HRP20170731T1 (hr) 2017-07-28
ES2627957T3 (es) 2017-08-01
EP3190109B1 (en) 2020-02-19
EA025086B1 (ru) 2016-11-30
US20160324828A1 (en) 2016-11-10
JP6116245B2 (ja) 2017-04-19
EP3190109A1 (en) 2017-07-12
AU2010258566B2 (en) 2015-05-14
EP2440550A1 (en) 2012-04-18
US20140066457A1 (en) 2014-03-06
US20120083475A1 (en) 2012-04-05
EP2440550B1 (en) 2017-03-15

Similar Documents

Publication Publication Date Title
EA025086B9 (ru) Производные индоламида и родственные соединения для использования при лечении нейродегенеративных заболеваний
GB201021104D0 (en) Novel compounds for the treatment of neurodegenerative diseases
TN2013000285A1 (en) Novel heterocyclic derivatives and their use in the treatment of neurological disorders
MX2008013212A (es) 4-anilinquinolina-3-carboxamidas como inhibidores de la cinsa csf-1r.
MX2013011908A (es) Composiciones y usos terapeuticos de inhibidores de cinasa epsilon relacionados con cinasa i-kappa b (ikk) y cinasa 1 de union tank.
MX2009004908A (es) Compuestos quimicos.
MX2014004479A (es) Derivados de oxazina novedosos y su uso en el tratamiento de enfermedades.
MY160052A (en) Alkoxy compounds for disease treatment
TN2012000249A1 (en) Pyrazine derivatives and their use in the treatment of neurological disorders
TN2012000231A1 (en) Quinoline amide m1 receptor positive allosteric modulators
MX2012006730A (es) Tiazolidinadionas moderadoras de receptores activados por proliferador de peroxizoma (ppar) y combinaciones para tratamiento de enfermedades neurodegenerativas y otras enfermedades metabolicas.
MY179527A (en) Catecholamine derivatives useful for the treatment of parkinson's disease
UA104489C2 (ru) Соединения для лечения дислипидемии и родственных болезней
WO2011127333A3 (en) Compounds for treating disease, for administering, and for pharmaceutical compositions
WO2009025785A3 (en) Cb2 receptor ligands for the treatment of pain
GEP20135806B (en) Lactams as beta secretase inhibitors
WO2008097924A3 (en) Pharmaceutical compositions comprising dextromethorphan analogs for the treatment of neurological disorders
BR112014001908A2 (pt) derivados aza heterocíclicos substituídos
WO2009036996A3 (en) Small molecule bradykinin b1 receptor antagonists
UA101393C2 (ru) КОМПОЗИЦИИ И ПРИМЕНЕНИЕ ПРОИЗВОДНЫХ ТРИАЗОЛА ДЛЯ ЛЕЧЕНИЯ β-АМИЛОИДОЗОВ И СИНУКЛЕИНОПАТИЙ
MX2010003269A (es) Derivados de pirrolotriazina utiles para tratar cancer a traves de la inhibicion de la aurora quinasa.
TW200734324A (en) Therapeutic agents
MX2009007889A (es) Derivados de 3-cinnolincarboxamida y su uso para el tratamiento del cancer.
MX2009013482A (es) Derivados de [1,10]-fenantrolina para el tratamiento de enfermedades neurodegenerativas o hematologicas.
MX2010008706A (es) Derivados de fenil-prenilo, de origen marino y sintetico. para el tratamiento de enfermedades o trastornos cognitivos, neurodegenerativos o neuronales.

Legal Events

Date Code Title Description
TH4A Publication of the corrected specification to eurasian patent
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM