JP6466970B2 - フェノール性ヒドロキシル基を介して連結された医薬的に活性な二量体 - Google Patents

フェノール性ヒドロキシル基を介して連結された医薬的に活性な二量体 Download PDF

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JP6466970B2
JP6466970B2 JP2016565186A JP2016565186A JP6466970B2 JP 6466970 B2 JP6466970 B2 JP 6466970B2 JP 2016565186 A JP2016565186 A JP 2016565186A JP 2016565186 A JP2016565186 A JP 2016565186A JP 6466970 B2 JP6466970 B2 JP 6466970B2
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dimer
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acid
naloxone
buprenorphine
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JP2017513917A5 (OSRAM
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シング ニキルシュ
シング ニキルシュ
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オーフォームド,インコーポレイティド
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    • C07C217/64Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
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JP2016565186A 2014-04-28 2015-04-27 フェノール性ヒドロキシル基を介して連結された医薬的に活性な二量体 Expired - Fee Related JP6466970B2 (ja)

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US201461985207P 2014-04-28 2014-04-28
US61/985,207 2014-04-28
US201562101768P 2015-01-09 2015-01-09
US201562176883P 2015-01-09 2015-01-09
US62/101,768 2015-01-09
US62/176,883 2015-01-09
PCT/US2015/027781 WO2015168014A1 (en) 2014-04-28 2015-04-27 Pharmaceutically active dimers linked through phenolic hydroxyl groups

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JP2017513917A JP2017513917A (ja) 2017-06-01
JP2017513917A5 JP2017513917A5 (OSRAM) 2018-06-14
JP6466970B2 true JP6466970B2 (ja) 2019-02-06

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JP2016565239A Expired - Fee Related JP6568102B2 (ja) 2014-04-28 2015-04-27 ブプレノルフィン二量体及び消化管疾患の治療におけるその使用

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017513918A (ja) * 2014-04-28 2017-06-01 オーフォームド,インコーポレイティド ブプレノルフィン二量体及び消化管疾患の治療におけるその使用

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108289869B (zh) * 2014-04-28 2021-08-27 奥佛麦德公司 使用通过酚羟基连接的药学活性的对乙酰氨基酚二聚体治疗疼痛的方法
EP3389628A4 (en) 2015-12-19 2019-08-07 Dixit, Manesh A. PHARMACEUTICAL FORMULATIONS OF MOUSE CHEESE TABLETS
US20190022013A1 (en) 2015-12-19 2019-01-24 First Time Us Generics Llc Soft-chew tablet pharmaceutical formulations
US20210113457A1 (en) 2018-02-02 2021-04-22 Ripple Therapeutics Corporation Glass formulations and uses thereof
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited Naphthylenyl compounds for long-acting injectable compositions and related methods
WO2020012245A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Thienothiophene-naltrexone prodrugs for long-acting injectable compositions
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds for long-acting injectable compositions and related methods
US12473326B2 (en) 2019-02-01 2025-11-18 Ripple Therapeutics Corporation Crystalline forms of dexamethasone dimers and uses thereof
US11236067B2 (en) 2019-07-12 2022-02-01 Orphomed, Inc. Compound for treating cystic fibrosis
WO2021024041A1 (en) * 2019-08-07 2021-02-11 Ripple Therapeutics Corporation Controlled release drug dimers
CN115956083A (zh) 2020-05-01 2023-04-11 波纹疗法公司 异二聚体组合物及用于治疗眼部病症的方法
WO2021262763A1 (en) * 2020-06-23 2021-12-30 Arriba Biopharma, Inc. Opioid receptor modulator and use thereof
CA3259656A1 (en) 2022-06-22 2023-12-28 Teva Czech Industries S.R.O SOLID FORMS OF DIBUPENORPHINE ETHYL ETHER AND THEIR PREPARATION PROCESS
WO2025014912A1 (en) * 2023-07-10 2025-01-16 Dimerx, Inc. Treatment of chronic pain or gastrointestinal disorders using buprenorphine dimer

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3896235A (en) * 1970-09-01 1975-07-22 Burroughs Wellcome Co Anthelmintic ethers and composition thereof
US5716631A (en) 1995-09-29 1998-02-10 Rdn Therapeutics Inc. Long acting narcotic analgesics and antagonists
SI1436012T1 (en) * 2001-10-18 2018-03-30 Nektar Therapeutics Polymer conjugates of opioid antagonists
WO2004039317A2 (en) 2002-10-25 2004-05-13 Euro-Celtique S.A. Analogs and prodrugs of buprenorphine
CN1263760C (zh) * 2002-11-12 2006-07-12 财团法人奇美医院 新颖的丁丙诺啡酯衍生物及其制备方法,以及长效作用镇痛药学组合物
DE60224288T2 (de) 2002-11-25 2009-04-16 Chi Mei Foundation Medical Center Buprenorphinesterderivate, Verfahren zu ihrer Herstellung, und langwirksame analgetische Arzneimittel
JP2004175706A (ja) * 2002-11-26 2004-06-24 Chi Mei Foundation Medical Center 新規なブプレノルフィンのエステル誘導体及びそれらの調製方法、及び長時間効力持続性鎮痛薬剤組成物
WO2004103317A2 (en) 2003-05-15 2004-12-02 Euro-Celtique S.A. Transdermal buprenorphine dosage regimen for treatment of diarrhea
WO2005009377A2 (en) * 2003-07-23 2005-02-03 University Of Kentucky Research Foundation Novel oral bioavailable prodrugs
CA2609810C (en) 2005-06-06 2012-05-22 Camurus Ab Glp-1 analogue formulations
US8852638B2 (en) 2005-09-30 2014-10-07 Durect Corporation Sustained release small molecule drug formulation
DK2001456T3 (da) 2006-04-04 2010-04-12 Emodys Gmbh Anvendelse af kappa-opiodreceptorantagonistholde sammensætninger til behandling af dissociative forstyrrelser
CN101466381B (zh) 2006-04-21 2012-11-14 尼克塔治疗公司 吗啡酮的立体选择性还原
MY156913A (en) 2008-05-07 2016-04-15 Nektar Therapeutics Oral administration of peripherally-acting opioid antagonists
US20100068786A1 (en) 2008-09-16 2010-03-18 Chmielewski Jean A Methods and compositions for reversing p-glycoprotein medicated drug resistance
US8461171B2 (en) * 2010-02-09 2013-06-11 QRxPharma Ltd. Hybrid opioid compounds and compositions
GB2513267B (en) 2010-06-08 2015-03-18 Rb Pharmaceuticals Ltd Injectable flowable composition comprising buprenorphine
KR101793101B1 (ko) 2010-08-20 2017-11-02 닥터 레디스 래보러토리즈 에스에이 인지질 데포
CN103289075B (zh) * 2012-02-22 2016-01-20 天津键凯科技有限公司 聚乙二醇与纳洛酮的结合物及其药物组合物和应用
PT3137081T (pt) * 2014-04-28 2018-02-08 Orphomed Inc Dímero de buprenorfina e o seu uso no tratamento de transtornos gastrointestinais

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017513918A (ja) * 2014-04-28 2017-06-01 オーフォームド,インコーポレイティド ブプレノルフィン二量体及び消化管疾患の治療におけるその使用

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