KR20180104123A - 비알콜성 지방간염 (NASH)의 치료를 위한 sGC 자극제의 용도 - Google Patents

비알콜성 지방간염 (NASH)의 치료를 위한 sGC 자극제의 용도 Download PDF

Info

Publication number
KR20180104123A
KR20180104123A KR1020187024680A KR20187024680A KR20180104123A KR 20180104123 A KR20180104123 A KR 20180104123A KR 1020187024680 A KR1020187024680 A KR 1020187024680A KR 20187024680 A KR20187024680 A KR 20187024680A KR 20180104123 A KR20180104123 A KR 20180104123A
Authority
KR
South Korea
Prior art keywords
alkyl
ring
membered heterocyclic
phenyl
membered heteroaryl
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.)
Ceased
Application number
KR1020187024680A
Other languages
English (en)
Korean (ko)
Inventor
지-윤 제이미 임
마크 지. 커리
제임스 에드워드 쉐펙
폴 앨런 렌하우
페이 제
제이미 엘. 매스페러
Original Assignee
아이언우드 파마슈티컬스, 인코포레이티드
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 아이언우드 파마슈티컬스, 인코포레이티드 filed Critical 아이언우드 파마슈티컬스, 인코포레이티드
Publication of KR20180104123A publication Critical patent/KR20180104123A/ko
Ceased legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • 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)
KR1020187024680A 2016-02-01 2017-01-31 비알콜성 지방간염 (NASH)의 치료를 위한 sGC 자극제의 용도 Ceased KR20180104123A (ko)

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
KR20180104123A true KR20180104123A (ko) 2018-09-19

Family

ID=58018271

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187024680A Ceased KR20180104123A (ko) 2016-02-01 2017-01-31 비알콜성 지방간염 (NASH)의 치료를 위한 sGC 자극제의 용도

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

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
WO2008124505A2 (en) * 2007-04-05 2008-10-16 Ironwood Pharmaceuticals,Inc. Soluble guanylate cyclase (sgc) modulators for treatment of lipid related disorders
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
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
ES2911276T3 (es) * 2013-03-15 2022-05-18 Cyclerion Therapeutics Inc Estimuladores de sGC
WO2015106268A1 (en) * 2014-01-13 2015-07-16 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
US9663527B2 (en) * 2014-02-11 2017-05-30 Merck Sharp & Dohme Corp. Factor XIa inhibitors
AU2015292833B2 (en) * 2014-07-22 2019-11-28 Boehringer Ingelheim International Gmbh Heterocyclic carboxylic acids as activators of soluble guanylate cyclase
BR112018011154B1 (pt) * 2015-11-30 2023-09-26 Cyclerion Therapeutics, Inc Dispersões sólidas compreendendo um estimulador de sgc
US11357777B2 (en) 2016-02-01 2022-06-14 Cyclerion Therapeutics, Inc. Use of sGC stimulators for the treatment of nonalcoholic steatohepatitis (NASH)
US10925876B2 (en) 2016-05-18 2021-02-23 Merck Sharp & Dohme Corp. Methods for using triazolo-pyrazinyl soluble guanylate cyclase activators in fibrotic disorders

Also Published As

Publication number Publication date
US11357777B2 (en) 2022-06-14
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
AU2017216429B2 (en) 2022-10-06

Similar Documents

Publication Publication Date Title
EP3411026B1 (en) Use of stimulators of soluble guanylate cyclase for the treatment of nonalcoholic steatohepatitis (nash)
JP7628096B2 (ja) 縮合二環式sgc刺激剤
JP7542518B2 (ja) ミトコンドリア(mitochonrial)障害の処置のためのsGC刺激剤の使用
JP7150740B2 (ja) sGC刺激薬による中枢神経系疾患の治療
EP3094327A1 (en) USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
KR20180094965A (ko) 위장 괄약근 기능장애의 치료를 위한 sGC 자극제의 용도
WO2018111795A2 (en) Use of sgc stimulators for the treatment of esophageal motility disorders
EA038096B1 (ru) ПРИМЕНЕНИЕ СТИМУЛЯТОРОВ sGC ДЛЯ ЛЕЧЕНИЯ НЕАЛКОГОЛЬНОГО СТЕАТОГЕПАТИТА (NASH)
HK40001613B (en) Use of stimulators of soluble guanylate cyclase for the treatment of nonalcoholic steatohepatitis (nash)
US20240342187A1 (en) Use of nep inhibitors for the treatment of gastrointestinal sphincter disorders
EA047256B1 (ru) ПРИМЕНЕНИЕ рГЦ СТИМУЛЯТОРОВ ДЛЯ ЛЕЧЕНИЯ МИТОХОНДРИАЛЬНЫХ ЗАБОЛЕВАНИЙ
BR112019004468B1 (pt) Estimulantes de sgc

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20180828

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
N231 Notification of change of applicant
PN2301 Change of applicant

Patent event date: 20190710

Comment text: Notification of Change of Applicant

Patent event code: PN23011R01D

A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20220125

Comment text: Request for Examination of Application

PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20240623

Patent event code: PE09021S01D

E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20240902

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D