BR112020015743A2 - Derivados de tiofeno não fundido e seus usos - Google Patents

Derivados de tiofeno não fundido e seus usos Download PDF

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Publication number
BR112020015743A2
BR112020015743A2 BR112020015743-0A BR112020015743A BR112020015743A2 BR 112020015743 A2 BR112020015743 A2 BR 112020015743A2 BR 112020015743 A BR112020015743 A BR 112020015743A BR 112020015743 A2 BR112020015743 A2 BR 112020015743A2
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BR
Brazil
Prior art keywords
optionally substituted
compound
alkyl
thiophene
disease
Prior art date
Application number
BR112020015743-0A
Other languages
English (en)
Portuguese (pt)
Inventor
Eric MELDRUM
Benoît de Chassey
Peter Machin
Karine Fabienne Malagu
Paul Colin Michael Winship
Jean-Laurent Paparin
Mark Chambers
Jamie David Knight
Roberta LANARO
Original Assignee
Enyo Pharma
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 Enyo Pharma filed Critical Enyo Pharma
Publication of BR112020015743A2 publication Critical patent/BR112020015743A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30Oxygen or sulfur atoms
    • C07D233/32One oxygen atom
    • C07D233/38One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535Heterocyclic 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
    • 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
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • 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
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D413/02Heterocyclic 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
BR112020015743-0A 2018-02-08 2019-02-08 Derivados de tiofeno não fundido e seus usos BR112020015743A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18305134 2018-02-08
EP18305134.1 2018-02-08
PCT/EP2019/053081 WO2019154956A1 (en) 2018-02-08 2019-02-08 Non-fused thiophene derivatives and their uses

Publications (1)

Publication Number Publication Date
BR112020015743A2 true BR112020015743A2 (pt) 2020-12-15

Family

ID=61283124

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112020015743-0A BR112020015743A2 (pt) 2018-02-08 2019-02-08 Derivados de tiofeno não fundido e seus usos

Country Status (15)

Country Link
US (2) US11840527B2 (https=)
EP (2) EP3749649A1 (https=)
JP (1) JP7399110B2 (https=)
KR (2) KR102871188B1 (https=)
CN (1) CN111936471B (https=)
AU (1) AU2019219123B2 (https=)
BR (1) BR112020015743A2 (https=)
CA (1) CA3087830A1 (https=)
CO (1) CO2020009106A2 (https=)
EA (1) EA202091897A1 (https=)
IL (1) IL275893B2 (https=)
MX (1) MX2020007917A (https=)
PH (1) PH12020551175A1 (https=)
SG (1) SG11202006723SA (https=)
WO (2) WO2019154953A1 (https=)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA202091889A1 (ru) 2018-02-08 2020-10-29 Энио Фарма Конденсированные производные тиофена и их применение
CA3087830A1 (en) 2018-02-08 2019-08-15 Enyo Pharma Non-fused thiophene derivatives and their uses
WO2021074357A1 (en) 2019-10-17 2021-04-22 Enyo Pharma Thiophene derivatives for use in treating portal inflammation and fibrosis
BR112022010924A2 (pt) 2019-12-06 2022-09-06 Vertex Pharma Tetra-hidrofuranos substituídos como moduladores de canais de sódio
KR20250133471A (ko) 2020-02-18 2025-09-05 길리애드 사이언시즈, 인코포레이티드 항바이러스 화합물
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
EP4185381A4 (en) * 2020-07-24 2024-08-21 Inipharm, Inc. Thiophene hsd17b13 inhibitors and uses thereof
CN116056695A (zh) 2020-08-05 2023-05-02 埃尼奥制药公司 治疗慢性肾病的方法
AU2021377248B2 (en) 2020-11-13 2025-12-18 Inipharm, Inc. Dichlorophenol hsd17b13 inhibitors and uses thereof
CN112851633B (zh) * 2021-01-19 2021-12-07 上海应用技术大学 一种2-氨基噻吩类神经氨酸酶抑制剂及其制备方法与应用
CA3216162A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
SMT202500481T1 (it) 2021-06-04 2026-01-12 Vertex Pharma N-(idrossialchil(etero)aril)tetraidrofuran carbossammidi come modulatori di canali del sodio
AU2022328698B2 (en) 2021-08-18 2025-02-20 Gilead Sciences, Inc. Phospholipid compounds and methods of making and using the same
WO2024037604A1 (zh) * 2022-08-17 2024-02-22 彭光浩 基于多种碳氮代谢途径的分枝杆菌、分离方法及用途

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GB9924092D0 (en) 1999-10-13 1999-12-15 Zeneca Ltd Pyrimidine derivatives
US20050085531A1 (en) * 2003-10-03 2005-04-21 Hodge Carl N. Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
DE10359791A1 (de) 2003-12-19 2005-07-21 Bayer Healthcare Ag Substituierte Thiophene
US8263641B2 (en) * 2007-09-10 2012-09-11 Calcimedica, Inc. Compounds that modulate intracellular calcium
US8389567B2 (en) 2007-12-12 2013-03-05 Calcimedica, Inc. Compounds that modulate intracellular calcium
TWI392673B (zh) 2008-08-27 2013-04-11 Calcimedica Inc 調控細胞內鈣離子濃度之化合物
US20110319416A1 (en) 2009-01-28 2011-12-29 Emory University Subunit Selective NMDA Receptor Antagonists For The Treatment Of Neurological Conditions
US20130085133A1 (en) * 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor anti-viral agent
WO2013142628A2 (en) * 2012-03-20 2013-09-26 Fred Hutchinson Cancer Research Center Antibiotic compounds and compositions, and methods for identification thereof
EP2679591A1 (en) * 2012-06-29 2014-01-01 Poxel Thienopyridone derivatives useful as activators of AMPK
WO2015187827A1 (en) 2014-06-03 2015-12-10 The Trustees Of The University Of Pennsylvania Novel effective antiviral compounds and methods using same
CN106687446B (zh) 2014-07-18 2020-04-28 百济神州(北京)生物科技有限公司 作为t790m/wt-egfr的选择性和不可逆的激酶抑制剂的5-氨基-4-氨甲酰基-吡唑化合物及其用途
EP3562818B1 (en) 2016-12-29 2022-05-18 ENYO Pharma Thiophene derivatives as antiviral agents
EA202091889A1 (ru) 2018-02-08 2020-10-29 Энио Фарма Конденсированные производные тиофена и их применение
CA3087830A1 (en) 2018-02-08 2019-08-15 Enyo Pharma Non-fused thiophene derivatives and their uses
US20210038566A1 (en) 2018-02-08 2021-02-11 Enyo Pharma Use of modulators of neet proteins for the treatment of infection

Also Published As

Publication number Publication date
CN111936471A (zh) 2020-11-13
WO2019154956A1 (en) 2019-08-15
CN111936471B (zh) 2024-10-29
IL275893A (en) 2020-08-31
US20210040059A1 (en) 2021-02-11
EP3749649A1 (en) 2020-12-16
CO2020009106A2 (es) 2020-10-30
JP7399110B2 (ja) 2023-12-15
WO2019154953A1 (en) 2019-08-15
AU2019219123B2 (en) 2022-12-08
KR20200141026A (ko) 2020-12-17
AU2019219123A1 (en) 2020-08-06
SG11202006723SA (en) 2020-08-28
KR102871188B1 (ko) 2025-10-15
US11840527B2 (en) 2023-12-12
MX2020007917A (es) 2020-10-28
EP3749650A1 (en) 2020-12-16
JP2021514385A (ja) 2021-06-10
US20200369655A1 (en) 2020-11-26
KR20240131460A (ko) 2024-08-30
EA202091897A1 (ru) 2020-10-27
IL275893B1 (en) 2024-04-01
CA3087830A1 (en) 2019-08-15
PH12020551175A1 (en) 2021-06-07
US11767316B2 (en) 2023-09-26
IL275893B2 (en) 2024-08-01

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B350 Update of information on the portal [chapter 15.35 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2813 DE 03-12-2024 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.