AU2018260535B2 - Small organic molecules for use in the treatment of neuroinflammatory disorders - Google Patents

Small organic molecules for use in the treatment of neuroinflammatory disorders Download PDF

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Publication number
AU2018260535B2
AU2018260535B2 AU2018260535A AU2018260535A AU2018260535B2 AU 2018260535 B2 AU2018260535 B2 AU 2018260535B2 AU 2018260535 A AU2018260535 A AU 2018260535A AU 2018260535 A AU2018260535 A AU 2018260535A AU 2018260535 B2 AU2018260535 B2 AU 2018260535B2
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bmp
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pharmaceutical composition
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AU2018260535A1 (en
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Karin Bernadet Fainberg
Arnon KARNI
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Medical Research Infrastructure and Health Services Fund of the Tel Aviv Medical Center
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Medical Research Infrastructure and Health Services Fund of the Tel Aviv Medical Center
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    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/345—Nitrofurans
    • 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • 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
    • A61K31/435—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2018260535A 2017-04-26 2018-04-26 Small organic molecules for use in the treatment of neuroinflammatory disorders Active AU2018260535B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IL251949A IL251949A0 (en) 2017-04-26 2017-04-26 Small organic molecules for use in the treatment of neuro-inflammatory diseases
IL251949 2017-04-26
PCT/IL2018/050463 WO2018198123A1 (en) 2017-04-26 2018-04-26 Small organic molecules for use in the treatment of neuroinflammatory disorders

Publications (2)

Publication Number Publication Date
AU2018260535A1 AU2018260535A1 (en) 2019-10-31
AU2018260535B2 true AU2018260535B2 (en) 2023-09-28

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018260535A Active AU2018260535B2 (en) 2017-04-26 2018-04-26 Small organic molecules for use in the treatment of neuroinflammatory disorders

Country Status (9)

Country Link
US (2) US11103479B2 (enExample)
EP (1) EP3615022B1 (enExample)
JP (1) JP6997800B2 (enExample)
CN (1) CN110869015B (enExample)
AU (1) AU2018260535B2 (enExample)
CA (1) CA3061296A1 (enExample)
ES (1) ES2948767T3 (enExample)
IL (2) IL251949A0 (enExample)
WO (1) WO2018198123A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019122202A1 (en) * 2017-12-20 2019-06-27 Ecole Polytechnique Federale De Lausanne (Epfl) Sting inhibitors
WO2019236890A1 (en) * 2018-06-07 2019-12-12 Disarm Therapeutics, Inc. Inhibitors of sarm1
US12083114B2 (en) * 2018-12-19 2024-09-10 Disarm Therapeutics, Inc. Inhibitors of SARM1 in combination with neuro-protective agents

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001023382A1 (en) * 1999-09-28 2001-04-05 Applied Research Systems Ars Holding N.V. Pharmaceutically active sulfonyl hydrazide derivatives
US20040039037A1 (en) * 2002-06-04 2004-02-26 Weijian Zhang Heterocyclic compounds and uses thereof
WO2008024302A2 (en) * 2006-08-21 2008-02-28 Synta Pharmaceuticals Corp. Compounds for treating proliferative disorders
WO2013186777A2 (en) * 2012-06-14 2013-12-19 The Medical Researth, Infrastructure, And Health Services Fund Of The Tel Aviv Medical Center Use of blocking agents of bone morphogenie protein (bmp) signaling for the treatment of neuroinflammatory and neurodegenerative diseases
WO2014160203A2 (en) * 2013-03-14 2014-10-02 The Brigham And Women's Hospital, Inc. Bmp inhibitors and methods of use thereof

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Publication number Priority date Publication date Assignee Title
MY109202A (en) 1992-07-10 1996-12-31 Nihon Nohyaku Co Ltd Isothiazole derivatives and processes for preparing the same as well as termite controlling agents comprising the same as active ingredient
IT1313601B1 (it) 1999-08-05 2002-09-09 Isagro Ricerca Srl Fenilpirazoli ad attivita' erbicida
US6727241B2 (en) 2002-06-12 2004-04-27 Chemocentryx Anti-inflammatory compositions and methods of use
GB0306357D0 (en) 2003-03-20 2003-04-23 Astrazeneca Ab Chemical compounds
US20080249038A1 (en) 2003-10-07 2008-10-09 Quark Biotech, Inc. Bone Morphogenetic Protein (Bmp) 2A and Uses Thereof
US20060217390A1 (en) 2005-02-24 2006-09-28 Esmir Gunic Cycloalkl, aryl and heteroaryl amino isothiazoles for the treatment of Hepatitis C virus
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
CN100396667C (zh) * 2006-02-20 2008-06-25 中国医学科学院医药生物技术研究所 一组具有上调骨形成蛋白bmp-2表达活性的五元不饱和杂环化合物
WO2008118626A2 (en) 2007-03-08 2008-10-02 Burnham Institute For Medical Research Inhibitors of jnk and methods for identifying inhibitors of jnk
CA2718403A1 (en) * 2008-03-13 2009-09-17 The General Hospital Corporation Inhibitors of the bmp signaling pathway
WO2011008640A1 (en) * 2009-07-14 2011-01-20 Beth Israel Deaconess Medical Center, Inc. Methods of increasing liver proliferation
KR20120081585A (ko) 2009-08-11 2012-07-19 알러간, 인코포레이티드 안질환을 치료하기 위한 이소티오졸
JP5725469B2 (ja) * 2010-11-15 2015-05-27 学校法人北里研究所 骨分化阻害剤およびその製造方法
JP6543342B2 (ja) 2014-08-14 2019-07-10 アルハマドシャー，マモウン，エム． 血清半減期を延長するための、調節可能リンカーを介した薬学的活性剤とトランスサイレチンリガンドのコンジュゲーション

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001023382A1 (en) * 1999-09-28 2001-04-05 Applied Research Systems Ars Holding N.V. Pharmaceutically active sulfonyl hydrazide derivatives
US20040039037A1 (en) * 2002-06-04 2004-02-26 Weijian Zhang Heterocyclic compounds and uses thereof
WO2008024302A2 (en) * 2006-08-21 2008-02-28 Synta Pharmaceuticals Corp. Compounds for treating proliferative disorders
WO2013186777A2 (en) * 2012-06-14 2013-12-19 The Medical Researth, Infrastructure, And Health Services Fund Of The Tel Aviv Medical Center Use of blocking agents of bone morphogenie protein (bmp) signaling for the treatment of neuroinflammatory and neurodegenerative diseases
WO2014160203A2 (en) * 2013-03-14 2014-10-02 The Brigham And Women's Hospital, Inc. Bmp inhibitors and methods of use thereof

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
BOERGERMANN J.H. et al. "Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells", THE INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY (2010) vol. 42, no. 11, 1 November 2010, pages 1802-1807 *
CHENG, X et al. "Bone morphogenetic protein signaling and olig1/2 interact to regulate the differentiation and maturation of adult oligodendrocyte precursor cells", STEM CELLS (2007) vol. 25, no. 12, pages 3204-3214 *
DATABASE CAS Database accession no. 882268-63-5 CA Index Name: 2-Thiophenecarboxylic acid, 3-[2- [cyano(2-thienylsulfonyl)methylene]hydrazinyl]-, methyl ester; 30 April 2006 *
DATABASE CAS Database accession no. 882278-00-4 "2-Thiophenecarboxylic acid, 4- cyano-3-[2-[cyano(2-thienylsulfonyl)methylene]hydrazinyl]-, methyl ester" 30 April 2006 *
DATABASE PubChem Database accession no. CID 2820255 "Methyl 3-[2-[cyano(thiophen-2-ylsulfonyl) methylidene]hydrazinyl]thiophene-2-carboxylate", 19 July 2005 *
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DATABASE PubChem Database accession no. CID 6376145 "Methyl 4-cyano-3-[(2E)-2-[cyano(thiophen-2- ylsulfonyl)methylidene]hydrazinyl]thiophene-2-carboxylate", 11 September 2005 *
HONG C.C. et al "Applications of small molecule BMP inhibitors in physiology and disease", CYTOKINE & GROWTH FACTOR REVIEWS (2009) vol. 20, no. 5-6, 1 October 2009 *
SANVITALE C.E. et al. "A new class of small molecule inhibitor of BMP signaling", PLOS ONE (2013) vol. 8, no. 4 pages e62721 *

Also Published As

Publication number Publication date
EP3615022A1 (en) 2020-03-04
CA3061296A1 (en) 2018-11-01
US20200046680A1 (en) 2020-02-13
US11779565B2 (en) 2023-10-10
IL251949A0 (en) 2017-07-31
EP3615022C0 (en) 2023-06-07
US20210393582A1 (en) 2021-12-23
EP3615022A4 (en) 2021-03-31
US11103479B2 (en) 2021-08-31
CN110869015B (zh) 2023-08-18
CN110869015A (zh) 2020-03-06
ES2948767T3 (es) 2023-09-18
JP2020517678A (ja) 2020-06-18
JP6997800B2 (ja) 2022-02-04
EP3615022B1 (en) 2023-06-07
WO2018198123A1 (en) 2018-11-01
AU2018260535A1 (en) 2019-10-31
IL269894B (en) 2022-03-01

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