CA3087830A1 - Non-fused thiophene derivatives and their uses - Google Patents

Non-fused thiophene derivatives and their uses Download PDF

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Publication number
CA3087830A1
CA3087830A1 CA3087830A CA3087830A CA3087830A1 CA 3087830 A1 CA3087830 A1 CA 3087830A1 CA 3087830 A CA3087830 A CA 3087830A CA 3087830 A CA3087830 A CA 3087830A CA 3087830 A1 CA3087830 A1 CA 3087830A1
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CA
Canada
Prior art keywords
optionally substituted
compound
alkyl
thiophene
disease
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3087830A
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English (en)
French (fr)
Inventor
Eric Meldrum
Benoit De Chassey
Peter Machin
Karine Fabienne MALAGU
Paul Colin Michael Winship
Jean-Laurent Paparin
Mark Chambers
Jamie David Knight
Roberta LANARO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Enyo Pharma SA
Original Assignee
Enyo Pharma SA
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 SA filed Critical Enyo Pharma SA
Publication of CA3087830A1 publication Critical patent/CA3087830A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic 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
    • C07D333/26—Heterocyclic 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/28—Heterocyclic 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C07D233/38—One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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)
CA3087830A 2018-02-08 2019-02-08 Non-fused thiophene derivatives and their uses Pending CA3087830A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18305134.1 2018-02-08
EP18305134 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
CA3087830A1 true CA3087830A1 (en) 2019-08-15

Family

ID=61283124

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3087830A Pending CA3087830A1 (en) 2018-02-08 2019-02-08 Non-fused thiophene derivatives and their uses

Country Status (15)

Country Link
US (2) US11767316B2 (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
BR112020015743A2 (pt) 2018-02-08 2020-12-15 Enyo Pharma Derivados de tiofeno não fundido e seus usos
MX2020007918A (es) 2018-02-08 2020-12-03 Enyo Pharma Derivados fusionados de tiofeno y sus usos.
CN114555577A (zh) * 2019-10-17 2022-05-27 埃尼奥制药公司 用于治疗门静脉炎症和纤维化的噻吩衍生物
CA3164134A1 (en) 2019-12-06 2021-06-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
AU2021224588B2 (en) 2020-02-18 2024-07-18 Gilead Sciences, Inc. Antiviral compounds
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
TWI794742B (zh) 2020-02-18 2023-03-01 美商基利科學股份有限公司 抗病毒化合物
WO2022020714A1 (en) * 2020-07-24 2022-01-27 Inipharm, Inc. Thiophene hsd17b13 inhibitors and uses thereof
EP4192448A1 (en) 2020-08-05 2023-06-14 ENYO Pharma Thiophen compounds for use in the treatment of renal fibrosis
CN116670118B (zh) 2020-11-13 2026-02-06 伊尼制药公司 二氯苯酚hsd17b13抑制剂及其用途
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
EP4323362B1 (en) 2021-04-16 2025-05-07 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
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
JP5411141B2 (ja) * 2007-09-10 2014-02-12 カルシメディカ，インク． 細胞内カルシウムを調節する化合物
US8389567B2 (en) 2007-12-12 2013-03-05 Calcimedica, Inc. Compounds that modulate intracellular calcium
US7906553B2 (en) * 2008-08-27 2011-03-15 Calcimedica, Inc. Substituted thiophene modulators of intracellular calcium
US20110319416A1 (en) 2009-01-28 2011-12-29 Emory University Subunit Selective NMDA Receptor Antagonists For The Treatment Of Neurological Conditions
WO2011097607A1 (en) * 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
US20150126519A1 (en) * 2012-03-20 2015-05-07 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
TW201607930A (zh) 2014-07-18 2016-03-01 百濟神州有限公司 作為ｔ７９０ｍ／ｗｔ－ｅｇｆｒ的選擇性和不可逆的激酶抑制劑的５－氨基－４－氨甲醯基－吡唑化合物及其用途
KR20190098204A (ko) 2016-12-29 2019-08-21 엔요 파마 항바이러스제로서의 티오펜 유도체
BR112020015743A2 (pt) 2018-02-08 2020-12-15 Enyo Pharma Derivados de tiofeno não fundido e seus usos
MX2020007918A (es) 2018-02-08 2020-12-03 Enyo Pharma Derivados fusionados de tiofeno y sus usos.
WO2019154958A1 (en) 2018-02-08 2019-08-15 Enyo Pharma Use of modulators of neet proteins for the treatment of infection

Also Published As

Publication number Publication date
US20210040059A1 (en) 2021-02-11
US11840527B2 (en) 2023-12-12
AU2019219123B2 (en) 2022-12-08
JP2021514385A (ja) 2021-06-10
KR20200141026A (ko) 2020-12-17
KR102871188B1 (ko) 2025-10-15
IL275893B2 (en) 2024-08-01
MX2020007917A (es) 2020-10-28
EP3749650A1 (en) 2020-12-16
WO2019154953A1 (en) 2019-08-15
AU2019219123A1 (en) 2020-08-06
IL275893B1 (en) 2024-04-01
EP3749649A1 (en) 2020-12-16
CN111936471A (zh) 2020-11-13
KR20240131460A (ko) 2024-08-30
US11767316B2 (en) 2023-09-26
PH12020551175A1 (en) 2021-06-07
BR112020015743A2 (pt) 2020-12-15
EA202091897A1 (ru) 2020-10-27
WO2019154956A1 (en) 2019-08-15
JP7399110B2 (ja) 2023-12-15
SG11202006723SA (en) 2020-08-28
IL275893A (en) 2020-08-31
CN111936471B (zh) 2024-10-29
US20200369655A1 (en) 2020-11-26
CO2020009106A2 (es) 2020-10-30

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