CN102822190B - 哺乳动物的类固醇代谢物 - Google Patents

哺乳动物的类固醇代谢物 Download PDF

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Publication number
CN102822190B
CN102822190B CN201080059467.3A CN201080059467A CN102822190B CN 102822190 B CN102822190 B CN 102822190B CN 201080059467 A CN201080059467 A CN 201080059467A CN 102822190 B CN102822190 B CN 102822190B
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China
Prior art keywords
compound
formula
compounds
acid
pharmaceutically acceptable
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Expired - Fee Related
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CN201080059467.3A
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English (en)
Chinese (zh)
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CN102822190A (zh
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斯科特·C·查普尔
大卫·S·卡西毕尔
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Eledon Pharmaceuticals Inc
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Tokai Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Nutrition Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CN201080059467.3A 2009-11-13 2010-11-09 哺乳动物的类固醇代谢物 Expired - Fee Related CN102822190B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26126209P 2009-11-13 2009-11-13
US61/261,262 2009-11-13
PCT/US2010/055996 WO2011059969A2 (en) 2009-11-13 2010-11-09 Mammalian metabolites of steroids

Publications (2)

Publication Number Publication Date
CN102822190A CN102822190A (zh) 2012-12-12
CN102822190B true CN102822190B (zh) 2016-03-30

Family

ID=43992357

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080059467.3A Expired - Fee Related CN102822190B (zh) 2009-11-13 2010-11-09 哺乳动物的类固醇代谢物

Country Status (8)

Country Link
US (2) US20120282331A1 (cg-RX-API-DMAC10.html)
EP (1) EP2499151A4 (cg-RX-API-DMAC10.html)
JP (1) JP5956928B2 (cg-RX-API-DMAC10.html)
CN (1) CN102822190B (cg-RX-API-DMAC10.html)
AU (1) AU2010319697B2 (cg-RX-API-DMAC10.html)
BR (1) BR112012012167A2 (cg-RX-API-DMAC10.html)
CA (1) CA2780365A1 (cg-RX-API-DMAC10.html)
WO (1) WO2011059969A2 (cg-RX-API-DMAC10.html)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100048524A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
EP2393827B1 (en) 2009-02-05 2015-10-07 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
PE20121048A1 (es) 2009-06-26 2012-08-25 Novartis Ag Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17
MX359399B (es) 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
CA2904170A1 (en) * 2013-03-14 2014-09-25 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
KR20160058774A (ko) 2013-08-12 2016-05-25 토카이 파마슈티컬, 아이엔씨. 안드로겐-표적 치료제를 이용하는 종양 질환 치료를 위한 바이오마커
WO2016054472A1 (en) 2014-10-02 2016-04-07 University Of Maryland, Baltimore Methods of treating pancreatic cancer
WO2016119742A1 (zh) * 2015-01-29 2016-08-04 苏州晶云药物科技有限公司 (3β)-17-(1H-苯并咪唑-1-基)雄甾-5，16-二烯-3-醇的盐及其制备方法
WO2017140183A1 (zh) * 2016-02-19 2017-08-24 深圳市塔吉瑞生物医药有限公司 一种取代的甾体类化合物及其应用
CN111454315B (zh) * 2020-04-15 2022-12-09 宁波第二激素厂 一种雄甾-16-烯-3β-醇的合成方法
CN116621902B (zh) * 2022-05-18 2026-03-27 湖南科益新生物医药有限公司 17-苯并咪唑基-10α-甲基-甾体衍生物及其制备方法、用途和药物组合物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101155823A (zh) * 2005-03-02 2008-04-02 马里兰州立大学 新的c-17-杂芳基甾族的cyp17抑制剂/抗雄激素物质：其合成，体外生物学活性，药代动力学和抗肿瘤活性
WO2009120565A2 (en) * 2008-03-25 2009-10-01 University Of Maryland, Baltimore Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
WO2010091299A2 (en) * 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel combination cancer therapies

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* Cited by examiner, † Cited by third party
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US3480621A (en) * 1967-01-17 1969-11-25 Phytogen Prod Inc Steroid ketal
ES2138618T3 (es) * 1992-03-31 2000-01-16 Btg Int Ltd Esteroides 17-sustituidos utiles en el tratamiento del cancer.
DE4232681C2 (de) * 1992-09-29 1994-11-24 Sigma Tau Ind Farmaceuti 17-Phenyl- und 17-Furyl-14beta,5alpha-androstan- und androsten- Derivate, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Zusammensetzung
GB2470873A (en) * 2008-03-12 2010-12-08 Univ Maryland Androgen receptor inactivation contributes to antitumor efficacy of CYP17 inhibitors in prostrate cancer

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101155823A (zh) * 2005-03-02 2008-04-02 马里兰州立大学 新的c-17-杂芳基甾族的cyp17抑制剂/抗雄激素物质：其合成，体外生物学活性，药代动力学和抗肿瘤活性
WO2009120565A2 (en) * 2008-03-25 2009-10-01 University Of Maryland, Baltimore Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
WO2010091299A2 (en) * 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel combination cancer therapies

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Androgen receptor inactivation contributes to antitumor efficacy of 17A-hydroxylase/17,20-lyase inhibitor 3B-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancer;Tadas Vasaitis 等;《Molecular Cancer Therapeutics》;20080831;第7卷(第8期);第2348-2357页 *
CYP17- and CYP11B-dependent steroid hydroxylases as drug development targets;Tarek Hakki 等;《Pharmacology & Therapeutics》;20060731;第111卷(第1期);第27-52页 *
Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens: Synthesis, in Vitro Biological Activity, Pharmacokinetics, and Antitumor Activity in the LAPC4 Human Prostate Cancer Xenograft Model;Venkatesh D. Handratta 等;《J. Med. Chem.》;20050325;第48卷(第8期);第2972-2984页 *

Also Published As

Publication number Publication date
AU2010319697A1 (en) 2012-06-07
WO2011059969A2 (en) 2011-05-19
EP2499151A2 (en) 2012-09-19
JP2013510856A (ja) 2013-03-28
US20170008920A1 (en) 2017-01-12
CN102822190A (zh) 2012-12-12
WO2011059969A3 (en) 2011-09-22
BR112012012167A2 (pt) 2017-10-03
EP2499151A4 (en) 2013-03-20
AU2010319697B2 (en) 2016-05-19
CA2780365A1 (en) 2011-05-19
JP5956928B2 (ja) 2016-07-27
US20120282331A1 (en) 2012-11-08

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