JP2016503030A - 医薬組成物 - Google Patents

医薬組成物 Download PDF

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Publication number
JP2016503030A
JP2016503030A JP2015548025A JP2015548025A JP2016503030A JP 2016503030 A JP2016503030 A JP 2016503030A JP 2015548025 A JP2015548025 A JP 2015548025A JP 2015548025 A JP2015548025 A JP 2015548025A JP 2016503030 A JP2016503030 A JP 2016503030A
Authority
JP
Japan
Prior art keywords
compound
isopropyl
cyclopenta
pentamethyl
dimethyl
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
JP2015548025A
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English (en)
Japanese (ja)
Other versions
JP2016503030A5 (enExample
Inventor
カイ，シェンシェン
ジョーンズ，ブライアン，アルヴィン
スパルテンステイン，アンドリュー
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.)
GlaxoSmithKline LLC
Original Assignee
GlaxoSmithKline LLC
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 GlaxoSmithKline LLC filed Critical GlaxoSmithKline LLC
Publication of JP2016503030A publication Critical patent/JP2016503030A/ja
Publication of JP2016503030A5 publication Critical patent/JP2016503030A5/ja
Pending legal-status Critical Current

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    • 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
    • A61K31/575—Compounds 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
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)
JP2015548025A 2012-12-14 2013-12-14 医薬組成物 Pending JP2016503030A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261737177P 2012-12-14 2012-12-14
US61/737,177 2012-12-14
PCT/US2013/075196 WO2014093941A1 (en) 2012-12-14 2013-12-14 Pharmaceutical compositions

Publications (2)

Publication Number Publication Date
JP2016503030A true JP2016503030A (ja) 2016-02-01
JP2016503030A5 JP2016503030A5 (enExample) 2017-02-02

Family

ID=50935020

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015548025A Pending JP2016503030A (ja) 2012-12-14 2013-12-14 医薬組成物

Country Status (20)

Country Link
US (2) US9795619B2 (enExample)
EP (1) EP2931285A4 (enExample)
JP (1) JP2016503030A (enExample)
KR (1) KR20150093819A (enExample)
CN (1) CN104902905A (enExample)
AU (1) AU2013358897B2 (enExample)
BR (1) BR112015013695A2 (enExample)
CA (1) CA2893959A1 (enExample)
CL (1) CL2015001660A1 (enExample)
CR (1) CR20150313A (enExample)
EA (1) EA201590862A1 (enExample)
HK (1) HK1209638A1 (enExample)
IL (1) IL238807A0 (enExample)
MA (1) MA38182A1 (enExample)
MX (1) MX2015007563A (enExample)
PE (1) PE20151326A1 (enExample)
PH (1) PH12015501156A1 (enExample)
SG (2) SG11201503807TA (enExample)
WO (1) WO2014093941A1 (enExample)
ZA (1) ZA201503594B (enExample)

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Publication number Priority date Publication date Assignee Title
JO3387B1 (ar) 2011-12-16 2019-03-13 Glaxosmithkline Llc مشتقات بيتولين
MA38182A1 (fr) * 2012-12-14 2018-04-30 Glaxosmithkline Llc Compositions pharmaceutiques a action prolongée pur une utilisation dans le traitement ou la prévention d'infections par le virus de l’immunodéficience humaine (vih)
DK3067358T3 (da) 2012-12-21 2019-11-04 Gilead Sciences Inc Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse
US9637516B2 (en) 2012-12-31 2017-05-02 Hetero Research Foundation Betulinic acid proline derivatives as HIV inhibitors
PL3019503T3 (pl) 2013-07-12 2018-01-31 Gilead Sciences Inc Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv
NO2865735T3 (enExample) 2013-07-12 2018-07-21
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
NO2717902T3 (enExample) 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
US20170129916A1 (en) 2014-06-26 2017-05-11 Hetero Research Foundation Novel betulinic proline imidazole derivatives as hiv inhibitors
SG11201702379TA (en) * 2014-09-26 2017-04-27 Glaxosmithkline Ip No 2 Ltd Long acting pharmaceutical compositions
TWI695003B (zh) 2014-12-23 2020-06-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
MA40886B1 (fr) 2015-02-09 2020-03-31 Hetero Research Foundation Nouveau triterpénone en c-3 avec des dérivés d'amide inverse en c-28 en tant qu'inhibiteurs du vih
US10370405B2 (en) 2015-03-16 2019-08-06 Hetero Labs Limited C-3 novel triterpenone with C-28 amide derivatives as HIV inhibitors
EP3277691B1 (en) 2015-04-02 2019-01-30 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
WO2018042331A1 (en) * 2016-08-31 2018-03-08 Glaxosmithkline Intellectual Property (No.2) Limited Combinations and uses and treatments thereof
WO2018042332A1 (en) * 2016-08-31 2018-03-08 Glaxosmithkline Intellectual Property (No.2) Limited Combinations and uses and treatments thereof
AU2018304591A1 (en) 2017-07-21 2020-03-05 Janssen Sciences Ireland Unlimited Company Regimens for treating hiv infections and aids

Citations (6)

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WO2008057420A2 (en) * 2006-11-03 2008-05-15 Panacos Pharmaceuticals, Inc. Extended triterpene derivatives
JP2010533148A (ja) * 2007-07-12 2010-10-21 テイボテク・フアーマシユーチカルズ （ｅ）４−［［４−［［４−（２−シアノエテニル）−２，６−ジメチルフェニル］アミノ］−２−ピリミジニル］アミノ］ベンゾニトリルの結晶形
JP2011508747A (ja) * 2008-01-03 2011-03-17 バイロケム ファーマ インコーポレイテッド 新規のｃ−２１ケトルパン誘導体、それらの調製および使用
WO2011100308A1 (en) * 2010-02-11 2011-08-18 Glaxosmithkline Llc Derivatives of betulin
WO2012037320A2 (en) * 2010-09-16 2012-03-22 Glaxosmithkline Llc Pharmaceutical compositions
WO2013090664A1 (en) * 2011-12-16 2013-06-20 Glaxosmithkline Llc Derivatives of betulin

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GB8815265D0 (en) 1988-06-27 1988-08-03 Wellcome Found Therapeutic nucleosides
US5358721A (en) * 1992-12-04 1994-10-25 Alza Corporation Antiviral therapy
EP1292562A1 (en) 2000-05-23 2003-03-19 Univerzita palackeho V Olomouci Triterpenoid derivatives
US7163700B2 (en) * 2001-07-31 2007-01-16 Capricorn Pharma, Inc. Amorphous drug beads
US20080206161A1 (en) * 2002-10-25 2008-08-28 Dov Tamarkin Quiescent foamable compositions, steroids, kits and uses thereof
US20050142205A1 (en) * 2003-07-18 2005-06-30 Julia Rashba-Step Methods for encapsulating small spherical particles prepared by controlled phase separation
WO2005112929A2 (en) 2004-05-20 2005-12-01 Cornell Research Foundation, Inc. Anti-hiv-1 activity of betulinol derivatives
TW200628161A (en) 2004-11-12 2006-08-16 Panacos Pharmaceuticals Inc Novel betulin derivatives, preparation thereof and use thereof
CN1682740A (zh) * 2005-03-11 2005-10-19 中国药科大学 五环三萜类化合物在制备糖原磷酸化酶抑制剂中的应用
WO2006105356A2 (en) 2005-03-29 2006-10-05 Regents Of The University Of Minnesota Methods of manufacturing bioactive 3-esters of betulinic aldehyde and betulinic acid
TWI457136B (zh) 2005-04-04 2014-10-21 Tibotec Pharm Ltd Ｈｉｖ-感染之預防
WO2006117666A2 (en) * 2005-04-29 2006-11-09 Pfizer Inc. Dosage forms, pharmaceutical compositions and methods for sub-tenon delivery
US20070197646A1 (en) 2006-02-21 2007-08-23 Achillion Pharmaceuticals, Inc. Substituted taraxastanes useful for treating viral infections
FI121468B (fi) 2006-06-07 2010-11-30 Valtion Teknillinen Betuliiniperäiset yhdisteet antimikrobisina aineina
HUE068406T2 (hu) 2006-06-23 2024-12-28 Janssen Sciences Ireland Unlimited Co A TMC278 vizes szuszpenziója
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WO2009082819A1 (en) 2008-01-03 2009-07-09 Virochem Pharma Inc. Novel lupane derivatives
DE102008037025C5 (de) * 2008-08-08 2016-07-07 Jesalis Pharma Gmbh Verfahren zur Herstellung kristalliner Wirkstoff-Mikropartikel bzw. einer Wirkstoffpartikel-Festkörperform
US8778990B2 (en) 2008-11-04 2014-07-15 Trustees Of Dartmouth College Betulinic acid derivatives and methods of use thereof
CZ301318B6 (cs) 2008-11-13 2010-01-13 Univerzita Palackého v Olomouci 2-Deoxyglykosidy triterpenoidu, zpusob jejich prípravy a jejich použití jako lécivo
EP3210603A1 (en) * 2008-12-11 2017-08-30 Shionogi & Co., Ltd Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
US8802727B2 (en) 2009-07-14 2014-08-12 Hetero Research Foundation, Hetero Drugs Limited Pharmaceutically acceptable salts of betulinic acid derivatives
US9067966B2 (en) 2009-07-14 2015-06-30 Hetero Research Foundation, Hetero Drugs Ltd. Lupeol-type triterpene derivatives as antivirals
WO2013020245A1 (en) 2011-08-08 2013-02-14 Glaxosmithkline Llc Carbonyl derivatives of betulin
WO2013020246A1 (en) 2011-08-08 2013-02-14 Glaxosmithkline Llc Methylene derivatives of betulin
ES2584684T3 (es) 2011-12-14 2016-09-28 Glaxosmithkline Llc Derivados de propenoato de betulina
WO2014035945A1 (en) 2012-08-28 2014-03-06 Glaxosmithkline Llc Pharmaceutical compositions
MA38182A1 (fr) * 2012-12-14 2018-04-30 Glaxosmithkline Llc Compositions pharmaceutiques a action prolongée pur une utilisation dans le traitement ou la prévention d'infections par le virus de l’immunodéficience humaine (vih)
SG11201702379TA (en) 2014-09-26 2017-04-27 Glaxosmithkline Ip No 2 Ltd Long acting pharmaceutical compositions

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008057420A2 (en) * 2006-11-03 2008-05-15 Panacos Pharmaceuticals, Inc. Extended triterpene derivatives
JP2010533148A (ja) * 2007-07-12 2010-10-21 テイボテク・フアーマシユーチカルズ （ｅ）４−［［４−［［４−（２−シアノエテニル）−２，６−ジメチルフェニル］アミノ］−２−ピリミジニル］アミノ］ベンゾニトリルの結晶形
JP2011508747A (ja) * 2008-01-03 2011-03-17 バイロケム ファーマ インコーポレイテッド 新規のｃ−２１ケトルパン誘導体、それらの調製および使用
WO2011100308A1 (en) * 2010-02-11 2011-08-18 Glaxosmithkline Llc Derivatives of betulin
WO2012037320A2 (en) * 2010-09-16 2012-03-22 Glaxosmithkline Llc Pharmaceutical compositions
WO2013090664A1 (en) * 2011-12-16 2013-06-20 Glaxosmithkline Llc Derivatives of betulin

Non-Patent Citations (1)

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Title
MED. CHEM. RES., vol. 20, JPN6017035715, 2011, pages 1247 - 1259, ISSN: 0003644120 *

Also Published As

Publication number Publication date
EA201590862A1 (ru) 2016-05-31
KR20150093819A (ko) 2015-08-18
CL2015001660A1 (es) 2015-10-02
PE20151326A1 (es) 2015-10-12
MA38182A1 (fr) 2018-04-30
AU2013358897A1 (en) 2015-07-02
SG11201503807TA (en) 2015-06-29
ZA201503594B (en) 2018-11-28
US9795619B2 (en) 2017-10-24
US20180042944A1 (en) 2018-02-15
SG10201704467SA (en) 2017-06-29
EP2931285A4 (en) 2016-06-01
US20150313917A1 (en) 2015-11-05
CN104902905A (zh) 2015-09-09
MX2015007563A (es) 2015-10-14
CR20150313A (es) 2015-10-19
PH12015501156A1 (en) 2015-08-10
CA2893959A1 (en) 2014-06-19
EP2931285A1 (en) 2015-10-21
HK1209638A1 (en) 2016-04-08
IL238807A0 (en) 2015-06-30
WO2014093941A1 (en) 2014-06-19
AU2013358897B2 (en) 2017-01-05
BR112015013695A2 (pt) 2017-07-11

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