TW202245795A - 合成之熊果酸衍生物及其使用方法 - Google Patents

合成之熊果酸衍生物及其使用方法 Download PDF

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Publication number
TW202245795A
TW202245795A TW111102086A TW111102086A TW202245795A TW 202245795 A TW202245795 A TW 202245795A TW 111102086 A TW111102086 A TW 111102086A TW 111102086 A TW111102086 A TW 111102086A TW 202245795 A TW202245795 A TW 202245795A
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Taiwan
Prior art keywords
heptamethyl
substituted
group
compound
alkyl
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TW111102086A
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English (en)
Chinese (zh)
Inventor
江昕
夏 都
孫海洲
米蓮恩 維斯尼克
羅伯特 M 二世 卡爾
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美商瑞塔醫藥有限責任公司
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Publication of TW202245795A publication Critical patent/TW202245795A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008Expansion of ring D by one atom, e.g. D homo steroids
    • 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06Anabolic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
TW111102086A 2021-01-18 2022-01-18 合成之熊果酸衍生物及其使用方法 TW202245795A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202163199694P 2021-01-18 2021-01-18
US63/199,694 2021-01-18

Publications (1)

Publication Number Publication Date
TW202245795A true TW202245795A (zh) 2022-12-01

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Application Number Title Priority Date Filing Date
TW111102086A TW202245795A (zh) 2021-01-18 2022-01-18 合成之熊果酸衍生物及其使用方法

Country Status (14)

Country Link
US (1) US20240140986A1 (https=)
EP (1) EP4277916A1 (https=)
JP (1) JP2024504637A (https=)
KR (1) KR20230147077A (https=)
CN (1) CN117015548A (https=)
AU (1) AU2022208727A1 (https=)
CA (1) CA3204434A1 (https=)
CL (1) CL2023002064A1 (https=)
CO (1) CO2023010422A2 (https=)
IL (1) IL304530A (https=)
MX (1) MX2023008454A (https=)
PE (1) PE20231661A1 (https=)
TW (1) TW202245795A (https=)
WO (1) WO2022155614A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN121794280A (zh) * 2023-07-28 2026-04-03 里亚塔医药控股有限责任公司 用于制备三萜类衍生物的方法

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* Cited by examiner, † Cited by third party
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BRPI0907423A2 (pt) 2008-01-11 2020-10-27 Reata Pharmaceuticals, Inc. composto triterpenoide sintético para uso em um método de melhoria da função renal em um indivíduo, e uso do referido composto
MX2010011439A (es) 2008-04-18 2011-01-25 Reata Pharmaceuticals Inc Moduladores de inflamacion antioxidantes: derivados del acido oleanolico homologacion c-17.
JP5529851B2 (ja) 2008-04-18 2014-06-25 リアタ ファーマシューティカルズ インコーポレイテッド 抗酸化炎症モジュレーター:c−17においてアミノ改変およびその他の改変を加えたオレアノール酸誘導体
KR101713140B1 (ko) * 2008-04-18 2017-03-08 리타 파마슈티컬스 잉크. C-환에서 포화된 산화방지성 염증 조절제 올레아놀산 유도체
US8071632B2 (en) 2008-04-18 2011-12-06 Reata Pharmaceuticals, Inc. Antioxidant inflammation modulators: novel derivatives of oleanolic acid
MX348862B (es) 2011-03-11 2017-07-03 Reata Pharmaceuticals Inc Derivados c4-monometil triterpenoides y sus metodos de uso.
TWI623548B (zh) * 2012-04-27 2018-05-11 瑞塔醫藥有限責任公司 齊墩果酸(bardoxolone methyl)之2,2-二氟基丙醯胺衍生物、多晶型及其使用方法
WO2013188818A1 (en) * 2012-06-15 2013-12-19 Reata Pharmaceuticals, Inc. A-ring epoxidized triterpenoid-based anti-inflammation modulators and methods of use thereof
JP6243428B2 (ja) * 2012-09-10 2017-12-06 リアタ ファーマシューティカルズ インコーポレイテッド オレアノール酸のc17−アルカンジイルおよびアルケンジイル誘導体ならびにその使用方法
US9512094B2 (en) 2012-09-10 2016-12-06 Reata Pharmaceuticals, Inc. C17-heteroaryl derivatives of oleanolic acid and methods of use thereof
SMT201700501T1 (it) 2012-09-10 2017-11-15 Reata Pharmaceuticals Inc Derivati c17-eteroarilici dell'acido oleanolico e metodi d'uso degli stessi
AR096046A1 (es) * 2013-04-24 2015-12-02 Abbvie Inc Derivados de 2,2-difluoropropanamida de metil bardoxolona, formas polimórficas y métodos de uso
JP7074674B2 (ja) * 2015-09-23 2022-05-24 リアタ ファーマシューティカルズ インコーポレイテッド Il-17の阻害及び他の使用のためのc4修飾オレアノール酸誘導体
CN110198718B (zh) * 2016-11-08 2023-01-10 里亚塔医药控股有限责任公司 使用甲基巴多索隆或其类似物治疗阿尔波特综合征的方法
MX2021003643A (es) * 2018-09-28 2021-08-19 Sichuan Haisco Pharmaceutical Co Ltd Derivados de terpenoides y usos de los mismos.

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Publication number Publication date
PE20231661A1 (es) 2023-10-17
KR20230147077A (ko) 2023-10-20
EP4277916A1 (en) 2023-11-22
CN117015548A (zh) 2023-11-07
MX2023008454A (es) 2023-08-07
IL304530A (en) 2023-09-01
JP2024504637A (ja) 2024-02-01
AU2022208727A1 (en) 2023-08-03
CL2023002064A1 (es) 2023-12-29
CA3204434A1 (en) 2022-07-21
US20240140986A1 (en) 2024-05-02
CO2023010422A2 (es) 2023-08-28
WO2022155614A1 (en) 2022-07-21

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