JP5956928B2 - 哺乳類のステロイドの代謝物質 - Google Patents

哺乳類のステロイドの代謝物質 Download PDF

Info

Publication number
JP5956928B2
JP5956928B2 JP2012538889A JP2012538889A JP5956928B2 JP 5956928 B2 JP5956928 B2 JP 5956928B2 JP 2012538889 A JP2012538889 A JP 2012538889A JP 2012538889 A JP2012538889 A JP 2012538889A JP 5956928 B2 JP5956928 B2 JP 5956928B2
Authority
JP
Japan
Prior art keywords
compound
formula
compounds
incubation
acid
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.)
Expired - Fee Related
Application number
JP2012538889A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013510856A (ja
JP2013510856A5 (enExample
Inventor
チャッペル,スコット,シー.
ケースビアー,デイビッド,エス.
Original Assignee
トーカイ ファーマシューティカルズ,インク.
トーカイ ファーマシューティカルズ,インク.
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 トーカイ ファーマシューティカルズ,インク., トーカイ ファーマシューティカルズ,インク. filed Critical トーカイ ファーマシューティカルズ,インク.
Publication of JP2013510856A publication Critical patent/JP2013510856A/ja
Publication of JP2013510856A5 publication Critical patent/JP2013510856A5/ja
Application granted granted Critical
Publication of JP5956928B2 publication Critical patent/JP5956928B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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)
JP2012538889A 2009-11-13 2010-11-09 哺乳類のステロイドの代謝物質 Expired - Fee Related JP5956928B2 (ja)

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 (3)

Publication Number Publication Date
JP2013510856A JP2013510856A (ja) 2013-03-28
JP2013510856A5 JP2013510856A5 (enExample) 2013-12-26
JP5956928B2 true JP5956928B2 (ja) 2016-07-27

Family

ID=43992357

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012538889A Expired - Fee Related JP5956928B2 (ja) 2009-11-13 2010-11-09 哺乳類のステロイドの代謝物質

Country Status (8)

Country Link
US (2) US20120282331A1 (enExample)
EP (1) EP2499151A4 (enExample)
JP (1) JP5956928B2 (enExample)
CN (1) CN102822190B (enExample)
AU (1) AU2010319697B2 (enExample)
BR (1) BR112012012167A2 (enExample)
CA (1) CA2780365A1 (enExample)
WO (1) WO2011059969A2 (enExample)

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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP5130453B2 (ja) * 2005-03-02 2013-01-30 ユニバーシティ オブ メリーランド,ボルティモア 新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性
GB2470873A (en) * 2008-03-12 2010-12-08 Univ Maryland Androgen receptor inactivation contributes to antitumor efficacy of CYP17 inhibitors in prostrate cancer
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

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
US20120282331A1 (en) 2012-11-08
CN102822190B (zh) 2016-03-30

Similar Documents

Publication Publication Date Title
JP2013510856A (ja) 哺乳類のステロイドの代謝物質
TWI439268B (zh) 雌激素受體調節劑及其用途
KR101819199B1 (ko) 안드로겐 수용체 조절제 및 이의 용도
KR100926399B1 (ko) 디아릴아민―함유 화합물 및 조성물, 및 스테로이드 호르몬핵 수용체의 조절제로서의 그들의 용도
JP2019031537A (ja) エストロゲン受容体調節剤としての6,7−ジヒドロ−5h−ベンゾ[7]アヌレン誘導体
JP5595402B2 (ja) アンドロゲン受容体モジュレーターとしての新規イミダゾリジン化合物
KR101036670B1 (ko) 헬릭스 12 유도된 비스테로이드성 항안드로겐
US8778958B2 (en) Synthesis of metabolically stable agents for alcohol and drug abuse
EP4066841A1 (en) Androgen receptor down-regulating agents and uses thereof
JP6842474B2 (ja) ステロイド系化合物、当該化合物を含む組成物及びその使用
TW200533641A (en) Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as orl1-receptor antagonists
JP5476587B2 (ja) エストロゲン受容体に対して活性を有する縮合化合物
US6689798B2 (en) Benzofuran derivatives
KR20200023362A (ko) 17.베타.-하이드록시스테로이드 탈수소효소의 억제제로 사용하기 위한 15.베타.-[3-프로판아미도]-치환된 에스트라-1,3,5(10)-트리엔-17-온 화합물 및 이의 17-옥심
EP3747881B1 (en) Nitrogen-containing benzoheterocycle compound comprising carboxylic acid group, preparation method and use thereof
JP6545266B2 (ja) 17β‐HSD1抑制剤のプロドラッグ
TW201512215A (zh) 治療活性雌三烯噻唑衍生物
Abdul-Rida et al. A novel pregnene analogs: synthesis, cytotoxicity on prostate cancer of PC-3 and LNCPa-AI cells and in silico molecular docking study
CZ207794A3 (en) Indole compounds, process of their preparation, intermediates and pharmaceutical compositions based thereon
US7732493B2 (en) 2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17β-hydroxy steroid dehydrogenase type 1
NL2031175B1 (en) Dhcr24 inhibitory compounds
Ledneczki et al. Discovery of novel steroid-based histamine H3 receptor antagonists/inverse agonists
CN107973780B (zh) 一种取代的烯烃类化合物及其制备方法和用途
CN112851741A (zh) 一种取代的甾体类化合物及其应用
JP2006517947A (ja) 抗腫瘍活性2−置換18a−ホモエストラ−1,3,5(10)−トリエン−3−イルスルファメート

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131108

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20131108

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20141112

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150209

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150810

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20151109

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151210

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20160518

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160617

R150 Certificate of patent or registration of utility model

Ref document number: 5956928

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees