CA2979203A1 - Inhibitors of short-chain dehydrogenase activity for treating fibrosis - Google Patents

Inhibitors of short-chain dehydrogenase activity for treating fibrosis

Info

Publication number
CA2979203A1
CA2979203A1 CA2979203A CA2979203A CA2979203A1 CA 2979203 A1 CA2979203 A1 CA 2979203A1 CA 2979203 A CA2979203 A CA 2979203A CA 2979203 A CA2979203 A CA 2979203A CA 2979203 A1 CA2979203 A1 CA 2979203A1
Authority
CA
Canada
Prior art keywords
alkyl
aryl
group
substituted
ch2x
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
CA2979203A
Other languages
English (en)
French (fr)
Inventor
Sanford Markowitz
Stanton Gerson
Amar Desai
Won Jin HO
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.)
Case Western Reserve University
Original Assignee
Case Western Reserve University
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 Case Western Reserve University filed Critical Case Western Reserve University
Publication of CA2979203A1 publication Critical patent/CA2979203A1/en
Pending legal-status Critical Current

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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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • 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
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2979203A 2015-03-08 2016-03-08 Inhibitors of short-chain dehydrogenase activity for treating fibrosis Pending CA2979203A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562129885P 2015-03-08 2015-03-08
US62/129,885 2015-03-08
PCT/US2016/021374 WO2016144958A1 (en) 2015-03-08 2016-03-08 Inhibitors of short-chain dehydrogenase activity for treating fibrosis

Publications (1)

Publication Number Publication Date
CA2979203A1 true CA2979203A1 (en) 2016-09-15

Family

ID=56879350

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2979203A Pending CA2979203A1 (en) 2015-03-08 2016-03-08 Inhibitors of short-chain dehydrogenase activity for treating fibrosis

Country Status (8)

Country Link
US (3) US10945998B2 (https=)
EP (1) EP3267995B1 (https=)
JP (3) JP2018511581A (https=)
CN (2) CN107921025A (https=)
AU (3) AU2016229918B2 (https=)
CA (1) CA2979203A1 (https=)
HK (1) HK1250636A1 (https=)
WO (1) WO2016144958A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11690847B2 (en) 2016-11-30 2023-07-04 Case Western Reserve University Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof
US11718589B2 (en) 2017-02-06 2023-08-08 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase
US12336982B2 (en) 2018-11-21 2025-06-24 Rodeo Therapeutics Corporation Compositions and methods of modulating short-chain dehydrogenase activity
US12616681B2 (en) 2022-08-22 2026-05-05 Case Western Reserve University Compositions and methods for treating renal injury

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DK2838533T3 (da) 2012-04-16 2017-11-27 Univ Case Western Reserve Sammensætninger og fremgangsmåder til at modulere 15-pgdh-aktivitet
US9801863B2 (en) 2012-04-16 2017-10-31 Case Western Reserve University Inhibitors of short-chain dehydrogenase activity for modulating hematopoietic stem cells and hematopoiesis
AU2014342811B2 (en) 2013-10-15 2019-01-03 Board Of Regents Of The University Of Texas System Compositions and methods of modulating short-chain dehydrogenase activity
CN107921025A (zh) 2015-03-08 2018-04-17 卡斯西部储备大学 用于治疗纤维症的短链脱氢酶活性的抑制剂
AU2016248080A1 (en) * 2015-04-14 2017-11-02 Board Of Regents Of The University Of Texas System Compositions and methods of modulating short-chain dehydrogenase activity
WO2018187810A1 (en) 2017-04-07 2018-10-11 Case Western Reserve University Inhibitors of short-chain dehydrogenase activity for treating coronary disorders
US20210317132A1 (en) * 2017-05-26 2021-10-14 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
TWI834795B (zh) 2019-01-08 2024-03-11 日商杏林製藥股份有限公司 15-pgdh抑制劑
EP3917911A1 (en) 2019-01-31 2021-12-08 Kyorin Pharmaceutical Co., Ltd. 15-pgdh inhibitors
KR20220146458A (ko) 2020-01-23 2022-11-01 마이오포르테 테라퓨틱스 인코포레이티드 Pgdh 억제제 및 그의 제조 및 사용 방법
JP2023515081A (ja) * 2020-02-21 2023-04-12 ケース ウエスタン リザーブ ユニバーシティ 腎損傷を治療するための組成物および方法
AU2021275122A1 (en) 2020-05-20 2022-12-15 Board Of Regents Of The University Of Texas System Compositions and methods of modulating short-chain dehydrogenase activity
EP4164638A4 (en) * 2020-06-11 2024-06-19 The Board of Trustees of the Leland Stanford Junior University REJUVENATION OF AGED TISSUES AND ORGANS BY INHIBITION OF THE DEGRADING ENZYME PGE2, 15-PGDH
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US20250002919A1 (en) * 2021-10-27 2025-01-02 The Board Of Trustees Of The Leland Stanford Junior University Regeneration or rejuvenation of tissues and organs
CN114875003B (zh) * 2022-04-06 2024-05-24 浙江大学 一种短链脱氢酶的突变体、编码基因及编码基因获得方法、突变体的应用
CN118027057A (zh) * 2022-11-14 2024-05-14 武汉人福创新药物研发中心有限公司 抑制15-pgdh的化合物及其用途
TW202434211A (zh) * 2023-02-17 2024-09-01 大陸商武漢人福創新藥物研發中心有限公司 亞碸類化合物及其用途
CN121772923A (zh) * 2023-06-28 2026-03-31 埃皮里姆生物股份有限公司 用于治疗与升高的15-pgdh相关的病况的间歇给药方法

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AU2016248080A1 (en) 2015-04-14 2017-11-02 Board Of Regents Of The University Of Texas System Compositions and methods of modulating short-chain dehydrogenase activity
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EP3548035A4 (en) 2016-11-30 2020-07-22 Case Western Reserve University COMBINATIONS OF 15-PGDH INHIBITORS WITH CORCOSTEROIDS AND / OR TNF INHIBITORS AND THEIR USES
JP2020514323A (ja) 2017-02-06 2020-05-21 ケース ウエスタン リザーブ ユニバーシティ 短鎖デヒドロゲナーゼ活性を調節する組成物と方法
WO2018187810A1 (en) 2017-04-07 2018-10-11 Case Western Reserve University Inhibitors of short-chain dehydrogenase activity for treating coronary disorders
JP2021134242A (ja) 2020-02-25 2021-09-13 株式会社アイティー技研 鉱物油精製方法及び装置
JP7574640B2 (ja) 2020-12-23 2024-10-29 株式会社リコー 画像処理装置、画像処理システム、方法およびプログラム

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US11690847B2 (en) 2016-11-30 2023-07-04 Case Western Reserve University Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof
US11718589B2 (en) 2017-02-06 2023-08-08 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase
US12336982B2 (en) 2018-11-21 2025-06-24 Rodeo Therapeutics Corporation Compositions and methods of modulating short-chain dehydrogenase activity
US12616681B2 (en) 2022-08-22 2026-05-05 Case Western Reserve University Compositions and methods for treating renal injury

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WO2016144958A1 (en) 2016-09-15
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CN107921025A (zh) 2018-04-17
AU2016229918A1 (en) 2017-09-28
US10945998B2 (en) 2021-03-16
HK1250636A1 (zh) 2019-01-11
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US20180064694A1 (en) 2018-03-08
EP3267995A1 (en) 2018-01-17
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US20210283113A1 (en) 2021-09-16
AU2021200610A1 (en) 2021-03-04
AU2022287625A1 (en) 2023-02-02
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US20250295640A1 (en) 2025-09-25
JP2021038247A (ja) 2021-03-11

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