AU2017216429B2 - Use of sGC stimulators for the treatment of Nonalcoholic Steatohepatitis (NASH) - Google Patents

Use of sGC stimulators for the treatment of Nonalcoholic Steatohepatitis (NASH) Download PDF

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Publication number
AU2017216429B2
AU2017216429B2 AU2017216429A AU2017216429A AU2017216429B2 AU 2017216429 B2 AU2017216429 B2 AU 2017216429B2 AU 2017216429 A AU2017216429 A AU 2017216429A AU 2017216429 A AU2017216429 A AU 2017216429A AU 2017216429 B2 AU2017216429 B2 AU 2017216429B2
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Australia
Prior art keywords
ring
alkyl
membered heterocyclic
phenyl
membered heteroaryl
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AU2017216429A
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AU2017216429A1 (en
Inventor
Mark G. Currie
Pei Ge
G-Yoon Jamie Im
Jaime L. Masferrer
Paul Allan Renhowe
James Edward SHEPPECK
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Cyclerion Therapeutics Inc
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Cyclerion Therapeutics Inc
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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
    • A61K31/395—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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/20—Milk; Whey; Colostrum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Mycology (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Developmental Biology & Embryology (AREA)
  • Virology (AREA)
  • Zoology (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)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
AU2017216429A 2016-02-01 2017-01-31 Use of sGC stimulators for the treatment of Nonalcoholic Steatohepatitis (NASH) Ceased AU2017216429B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662289463P 2016-02-01 2016-02-01
US62/289,463 2016-02-01
US201662398872P 2016-09-23 2016-09-23
US62/398,872 2016-09-23
PCT/US2017/015749 WO2017136309A1 (en) 2016-02-01 2017-01-31 USE OF sGC STIMULATORS FOR THE TREATMENT OF NONALCOHOLIC STEATOHEPATITIS (NASH)

Publications (2)

Publication Number Publication Date
AU2017216429A1 AU2017216429A1 (en) 2018-08-16
AU2017216429B2 true AU2017216429B2 (en) 2022-10-06

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Application Number Title Priority Date Filing Date
AU2017216429A Ceased AU2017216429B2 (en) 2016-02-01 2017-01-31 Use of sGC stimulators for the treatment of Nonalcoholic Steatohepatitis (NASH)

Country Status (11)

Country Link
US (1) US11357777B2 (enExample)
EP (1) EP3411026B1 (enExample)
JP (1) JP7098214B2 (enExample)
KR (1) KR20180104123A (enExample)
CN (2) CN116726178A (enExample)
AU (1) AU2017216429B2 (enExample)
BR (1) BR112018015718A2 (enExample)
CA (1) CA3012001A1 (enExample)
IL (1) IL260701B (enExample)
MX (1) MX386216B (enExample)
WO (1) WO2017136309A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10844064B2 (en) * 2014-09-17 2020-11-24 Cyclerion Therapeutics, Inc. sGC stimulators
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
US11357777B2 (en) 2016-02-01 2022-06-14 Cyclerion Therapeutics, Inc. Use of sGC stimulators for the treatment of nonalcoholic steatohepatitis (NASH)
CN110831593A (zh) * 2017-06-14 2020-02-21 特维娜有限公司 用于调节s1p1活性的化合物及其使用方法
WO2019055859A1 (en) * 2017-09-14 2019-03-21 Ironwood Pharmaceuticals, Inc. TREATMENT OF METABOLIC SYNDROME BY SGC STIMULATOR
US12220414B2 (en) * 2018-07-11 2025-02-11 Tisento Therapeutics Inc. Use of sGC stimulators for the treatment of mitochondrial disorders
AU2019301887A1 (en) * 2018-07-12 2021-01-07 Boehringer Ingelheim International Gmbh Alkoxy pyrazoles as soluble guanylate cyclase activators
WO2021073643A1 (zh) * 2019-10-18 2021-04-22 正大天晴药业集团股份有限公司 用于治疗非酒精性脂肪性肝炎的药物
MX2022005766A (es) 2019-11-19 2022-08-08 Trevena Inc Compuestos y métodos para la preparación de compuestos moduladores de esfingosina 1-fosfato tipo 1 (s1p1).
CA3170507A1 (en) * 2020-02-21 2021-08-26 Universiteit Maastricht Use of a soluble guanylate cyclase (sgc) stimulator or of a combination of a sgc stimulator and an sgc activator for conditions wherein the heme group of sgc is oxidized or wherein sgc is deficient in heme
CN118525022A (zh) * 2022-01-27 2024-08-20 西藏海思科制药有限公司 一种氮杂并环衍生物及其在医药上的应用

Citations (3)

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WO2008124505A2 (en) * 2007-04-05 2008-10-16 Ironwood Pharmaceuticals,Inc. Soluble guanylate cyclase (sgc) modulators for treatment of lipid related disorders
WO2014144100A2 (en) * 2013-03-15 2014-09-18 Takashi Nakai Sgc stimulators
WO2017095697A1 (en) * 2015-11-30 2017-06-08 Ironwood Pharmaceuticals, Inc. Solid dispersions comprising a sgc stimulator

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DE10109861A1 (de) 2001-03-01 2002-09-05 Bayer Ag Neuartige seitenkettenhalogenierte Aminodicarbonsäurederivate
CN102056907B (zh) 2008-04-04 2014-12-31 武田药品工业株式会社 杂环衍生物及其用途
US9260424B2 (en) * 2009-10-26 2016-02-16 Auspex Pharmaceuticals, Inc. 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase
DE102010021637A1 (de) * 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
ES2549979T3 (es) 2010-05-26 2015-11-03 Adverio Pharma Gmbh El uso de estimuladores de la sGC, activadores de la sGC, solos y en combinaciones con inhibidores de la PDE5 para el tratamiento de esclerosis sistémica (EcS)
US8569339B2 (en) 2011-03-10 2013-10-29 Boehringer Ingelheim International Gmbh Soluble guanylate cyclase activators
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WO2014144100A2 (en) * 2013-03-15 2014-09-18 Takashi Nakai Sgc stimulators
WO2017095697A1 (en) * 2015-11-30 2017-06-08 Ironwood Pharmaceuticals, Inc. Solid dispersions comprising a sgc stimulator

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US11357777B2 (en) 2022-06-14
KR20180104123A (ko) 2018-09-19
CN108697678A (zh) 2018-10-23
BR112018015718A2 (pt) 2019-01-08
AU2017216429A1 (en) 2018-08-16
IL260701A (enExample) 2018-09-20
CN116726178A (zh) 2023-09-12
JP2019507185A (ja) 2019-03-14
MX2018009173A (es) 2018-11-19
WO2017136309A1 (en) 2017-08-10
EP3411026A1 (en) 2018-12-12
MX386216B (es) 2025-03-18
US20210161893A1 (en) 2021-06-03
EP3411026B1 (en) 2022-03-09
CA3012001A1 (en) 2017-08-10
IL260701B (en) 2022-09-01
JP7098214B2 (ja) 2022-07-11

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