CA3012001A1 - 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
CA3012001A1
CA3012001A1 CA3012001A CA3012001A CA3012001A1 CA 3012001 A1 CA3012001 A1 CA 3012001A1 CA 3012001 A CA3012001 A CA 3012001A CA 3012001 A CA3012001 A CA 3012001A CA 3012001 A1 CA3012001 A1 CA 3012001A1
Authority
CA
Canada
Prior art keywords
ring
alkyl
membered heterocyclic
membered heteroaryl
phenyl
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
CA3012001A
Other languages
English (en)
French (fr)
Inventor
G-Yoon Jamie Im
Mark G. Currie
James Edward SHEPPECK
Paul Allan Renhowe
Pei Ge
Jaime L. Masferrer
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.)
Cyclerion Therapeutics Inc
Original Assignee
Ironwood Pharmaceuticals Inc
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 Ironwood Pharmaceuticals Inc filed Critical Ironwood Pharmaceuticals Inc
Publication of CA3012001A1 publication Critical patent/CA3012001A1/en
Pending legal-status Critical Current

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    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/53Heterocyclic 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
    • 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
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines 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
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/20Milk; Whey; Colostrum
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures 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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Zoology (AREA)
  • Developmental Biology & Embryology (AREA)
  • Cell Biology (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Mycology (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)
CA3012001A 2016-02-01 2017-01-31 Use of sgc stimulators for the treatment of nonalcoholic steatohepatitis (nash) Pending CA3012001A1 (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 (1)

Publication Number Publication Date
CA3012001A1 true CA3012001A1 (en) 2017-08-10

Family

ID=58018271

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3012001A Pending CA3012001A1 (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
AU2015317823A1 (en) * 2014-09-17 2017-03-23 Ironwood Pharmaceuticals, Inc. sGC stimulators
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
KR20180104123A (ko) 2016-02-01 2018-09-19 아이언우드 파마슈티컬스, 인코포레이티드 비알콜성 지방간염 (NASH)의 치료를 위한 sGC 자극제의 용도
JP7252908B2 (ja) * 2017-06-14 2023-04-05 トレベナ・インコーポレイテッド S1p1活性を調節するための化合物およびその使用法
WO2019055859A1 (en) * 2017-09-14 2019-03-21 Ironwood Pharmaceuticals, Inc. TREATMENT OF METABOLIC SYNDROME BY SGC STIMULATOR
BR112021000358A2 (pt) 2018-07-11 2021-04-06 Cyclerion Therapeutics, Inc. Uso de estimulantes de sgc para o tratamento de distúrbios mitocondriais
EA202190193A1 (ru) * 2018-07-12 2021-06-16 Бёрингер Ингельхайм Интернациональ Гмбх Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
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
US11884655B2 (en) 2019-11-19 2024-01-30 Trevena, Inc. Compounds and methods of preparing compounds S1P1 modulators
WO2021167458A1 (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

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10109861A1 (de) 2001-03-01 2002-09-05 Bayer Ag Neuartige seitenkettenhalogenierte Aminodicarbonsäurederivate
US20100144864A1 (en) 2007-04-05 2010-06-10 Ironwood Pharmaceuticals, Inc. Soluble guanylate cyclase (sgc) modulators for treatment of lipid related disorders
CA2720343A1 (en) 2008-04-04 2009-10-08 Takeda Pharmaceutical Company Limited Heterocyclic derivative and use thereof
US9260424B2 (en) 2009-10-26 2016-02-16 Auspex Pharmaceuticals, Inc. 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase
PL2576548T3 (pl) 2010-05-26 2015-11-30 Adverio Pharma Gmbh Zastosowanie stymulatorów sGC, aktywatorów sGC, pojedynczo i w kombinacjach z inhibitorami PDE5, w leczeniu twardziny układowej (SSc)
DE102010021637A1 (de) * 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
WO2012122340A1 (en) 2011-03-10 2012-09-13 Boehringer Ingelheim International Gmbh Soluble guanylate cyclase activators
CN102164320B (zh) 2011-04-11 2016-06-22 北京数字太和科技有限责任公司 一种改进的基于条件接收技术的终端
KR102362835B1 (ko) * 2013-03-15 2022-02-14 사이클리온 테라퓨틱스, 인크. sGC 자극인자
WO2015106268A1 (en) * 2014-01-13 2015-07-16 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
EP3104701B1 (en) * 2014-02-11 2019-01-30 Merck Sharp & Dohme Corp. Factor xia inhibitors
JP6602840B2 (ja) * 2014-07-22 2019-11-06 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 可溶性グアニル酸シクラーゼの活性化因子としてのヘテロ環式カルボン酸
KR102841419B1 (ko) 2015-11-30 2025-08-01 사이클리온 테라퓨틱스, 인크. sGC 자극제를 포함하는 고체 분산물
KR20180104123A (ko) 2016-02-01 2018-09-19 아이언우드 파마슈티컬스, 인코포레이티드 비알콜성 지방간염 (NASH)의 치료를 위한 sGC 자극제의 용도
WO2017200857A1 (en) 2016-05-18 2017-11-23 Merck Sharp & Dohme Corp. Methods for using triazolo-pyrazinyl soluble guanylate cyclase activators in fibrotic disorders

Also Published As

Publication number Publication date
IL260701A (enExample) 2018-09-20
CN116726178A (zh) 2023-09-12
IL260701B (en) 2022-09-01
KR20180104123A (ko) 2018-09-19
AU2017216429B2 (en) 2022-10-06
US11357777B2 (en) 2022-06-14
EP3411026B1 (en) 2022-03-09
CN108697678A (zh) 2018-10-23
JP2019507185A (ja) 2019-03-14
MX386216B (es) 2025-03-18
US20210161893A1 (en) 2021-06-03
MX2018009173A (es) 2018-11-19
BR112018015718A2 (pt) 2019-01-08
JP7098214B2 (ja) 2022-07-11
EP3411026A1 (en) 2018-12-12
WO2017136309A1 (en) 2017-08-10
AU2017216429A1 (en) 2018-08-16

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