JP6186012B2 - Ｃ−３アルキルおよびアルケニル修飾ベツリン酸誘導体 - Google Patents

Ｃ−３アルキルおよびアルケニル修飾ベツリン酸誘導体 Download PDF

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Publication number
JP6186012B2
JP6186012B2 JP2015558996A JP2015558996A JP6186012B2 JP 6186012 B2 JP6186012 B2 JP 6186012B2 JP 2015558996 A JP2015558996 A JP 2015558996A JP 2015558996 A JP2015558996 A JP 2015558996A JP 6186012 B2 JP6186012 B2 JP 6186012B2
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Japan
Prior art keywords
mmol
cyclopenta
pentamethyl
prop
alkyl
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Expired - Fee Related
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JP2015558996A
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English (en)
Japanese (ja)
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JP2016509062A (ja
JP2016509062A5 (cg-RX-API-DMAC7.html
Inventor
ジェイコブ・スウィドースキ
ヤン・チェン
シン−ユエン・シット
ニコラス・エイ・ミーンウェル
アリシア・レゲイロ−レン
チェン・ジエ
チェン・リウ
リチャード・エイ・ハーツ
リ・シュー
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.)
Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2015558996A 2013-02-25 2014-02-21 Ｃ−３アルキルおよびアルケニル修飾ベツリン酸誘導体 Expired - Fee Related JP6186012B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361768630P 2013-02-25 2013-02-25
US61/768,630 2013-02-25
PCT/US2014/017688 WO2014130810A1 (en) 2013-02-25 2014-02-21 C-3 alkyl and alkenyl modified betulinic acid derivatives useful in the treatment of hiv

Publications (3)

Publication Number Publication Date
JP2016509062A JP2016509062A (ja) 2016-03-24
JP2016509062A5 JP2016509062A5 (cg-RX-API-DMAC7.html) 2016-12-15
JP6186012B2 true JP6186012B2 (ja) 2017-08-23

Family

ID=50288267

Family Applications (1)

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JP2015558996A Expired - Fee Related JP6186012B2 (ja) 2013-02-25 2014-02-21 Ｃ−３アルキルおよびアルケニル修飾ベツリン酸誘導体

Country Status (15)

Country Link
US (1) US9249180B2 (cg-RX-API-DMAC7.html)
EP (1) EP2958930A1 (cg-RX-API-DMAC7.html)
JP (1) JP6186012B2 (cg-RX-API-DMAC7.html)
KR (1) KR20150121712A (cg-RX-API-DMAC7.html)
CN (1) CN105102468A (cg-RX-API-DMAC7.html)
AR (1) AR094876A1 (cg-RX-API-DMAC7.html)
AU (1) AU2014218754B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015019590A2 (cg-RX-API-DMAC7.html)
CA (1) CA2902513A1 (cg-RX-API-DMAC7.html)
EA (1) EA027861B1 (cg-RX-API-DMAC7.html)
IL (1) IL240739A0 (cg-RX-API-DMAC7.html)
MX (1) MX2015010354A (cg-RX-API-DMAC7.html)
SG (1) SG11201506445PA (cg-RX-API-DMAC7.html)
TW (1) TW201444862A (cg-RX-API-DMAC7.html)
WO (1) WO2014130810A1 (cg-RX-API-DMAC7.html)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
US20180094019A1 (en) * 2015-04-14 2018-04-05 ViiV Healthcare UK (No.4) Limited Crystalline forms of modified triterpenoid hydrochloride salts with hiv maturation inhibitor activity
EP3371171B1 (en) 2015-11-02 2023-10-25 Blueprint Medicines Corporation Inhibitors of ret
AR107512A1 (es) 2016-02-04 2018-05-09 VIIV HEALTHCARE UK Nº 5 LTD Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1
UY37155A (es) 2016-03-17 2017-10-31 Blueprint Medicines Corp Inhibidores de ret
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
US10035789B2 (en) 2016-07-27 2018-07-31 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
WO2018044838A1 (en) * 2016-08-31 2018-03-08 Viiv Healthcare Company Combinations and uses and treatments thereof
CN106749486A (zh) * 2016-11-30 2017-05-31 沈阳化工大学 一种以乙二胺为连接臂的齐墩果酸衍生物及其应用
RU2758376C2 (ru) 2017-09-14 2021-10-28 Феникс Байотекнолоджи, Инк. Способ и улучшенная нейропротекторная композиция для лечения неврологических патологических состояний
AU2018334386B2 (en) 2017-09-14 2021-11-04 Phoenix Biotechnology, Inc. Method and composition for treating viral infection
WO2019195471A1 (en) 2018-04-03 2019-10-10 Blueprint Medicines Corporation Ret inhibitor for use in treating cancer having a ret alteration
US12275712B2 (en) 2019-02-11 2025-04-15 Hetero Labs Limited Triterpene derivatives as HIV inhibitors
CN111362923A (zh) * 2020-03-25 2020-07-03 魏威 制备ret抑制剂普拉塞替尼的方法、以及普拉塞替尼的中间体及其制备方法
CN111440151A (zh) * 2020-03-25 2020-07-24 魏威 制备抗肿瘤药普拉赛替尼的方法
EP4009981B1 (en) 2020-03-31 2023-08-16 Phoenix Biotechnology, Inc. Method and compositions for treating coronavirus infection
SG11202105728YA (en) 2020-03-31 2021-11-29 Phoenix Biotechnology Inc Method and compositions for treating coronavirus infection
CA3183728A1 (en) 2020-05-29 2021-12-02 Blueprint Medicines Corporation Solid forms of pralsetinib

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5679828A (en) 1995-06-05 1997-10-21 Biotech Research Labs, Inc. Betulinic acid and dihydrobetulinic acid derivatives and uses therefor
US6369101B1 (en) * 1999-02-26 2002-04-09 Regents Of The University Of Minnesota Therapeutic method to treat herpes virus infection
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
US20040110785A1 (en) 2001-02-02 2004-06-10 Tao Wang Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
US7365221B2 (en) 2002-09-26 2008-04-29 Panacos Pharmaceuticals, Inc. Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof
US7745625B2 (en) 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
AU2005224260A1 (en) 2004-03-17 2005-09-29 Panacos Pharmaceuticals, Inc. Pharmaceuticals salts of 3-O-(3',3'-dimethylsuccinyl) betulinic acid
TW200628161A (en) 2004-11-12 2006-08-16 Panacos Pharmaceuticals Inc Novel betulin derivatives, preparation thereof and use thereof
US20110144069A1 (en) 2006-10-16 2011-06-16 Myriad Genetics, Incorporated Compounds for treating viral infections
CA2714049A1 (en) 2008-02-14 2009-08-20 Virochem Pharma Inc. Novel 17.beta. lupane derivatives
US9067966B2 (en) 2009-07-14 2015-06-30 Hetero Research Foundation, Hetero Drugs Ltd. Lupeol-type triterpene derivatives as antivirals
CA2801487C (en) * 2010-06-04 2017-12-05 Bristol-Myers Squibb Company Modified c-3 betulinic acid derivatives as hiv maturation inhibitors
RS54239B1 (sr) * 2010-06-04 2015-12-31 Bristol-Myers Squibb Company C-28 amidi modifikovanih derivata c-3 betulinske kiseline kao inhibitori sazrevanja hiv-a
CN103339141B (zh) 2011-01-31 2016-08-24 百时美施贵宝公司 作为hiv成熟抑制剂的c-3修饰的桦木酸衍生物的c-28胺
KR101886467B1 (ko) * 2011-01-31 2018-08-07 비브 헬스케어 유케이 (넘버4) 리미티드 Hiv 성숙 억제 활성을 갖는 c-17 및 c-3 변형 트리테르페노이드
US8889854B2 (en) 2012-05-07 2014-11-18 Bristol-Myers Squibb Company C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity

Also Published As

Publication number Publication date
US9249180B2 (en) 2016-02-02
MX2015010354A (es) 2015-10-09
EA027861B1 (ru) 2017-09-29
AR094876A1 (es) 2015-09-02
IL240739A0 (en) 2015-10-29
CA2902513A1 (en) 2014-08-28
US20140243298A1 (en) 2014-08-28
AU2014218754B2 (en) 2017-04-20
WO2014130810A1 (en) 2014-08-28
JP2016509062A (ja) 2016-03-24
EP2958930A1 (en) 2015-12-30
TW201444862A (zh) 2014-12-01
BR112015019590A2 (pt) 2017-07-18
EA201591545A1 (ru) 2015-12-30
AU2014218754A1 (en) 2015-10-15
SG11201506445PA (en) 2015-09-29
CN105102468A (zh) 2015-11-25
KR20150121712A (ko) 2015-10-29

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