KR20110081852A - 페놀성 오피오이드를 약독화시켜 방출하는 약제학적 조성물 - Google Patents

페놀성 오피오이드를 약독화시켜 방출하는 약제학적 조성물 Download PDF

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KR20110081852A
KR20110081852A KR1020117011102A KR20117011102A KR20110081852A KR 20110081852 A KR20110081852 A KR 20110081852A KR 1020117011102 A KR1020117011102 A KR 1020117011102A KR 20117011102 A KR20117011102 A KR 20117011102A KR 20110081852 A KR20110081852 A KR 20110081852A
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pharmaceutical composition
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토마스 이. 젠킨스
줄리에 디. 세루기
조나단 더블유. 레이
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파마코포어, 인크.
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    • C07K5/06Dipeptides
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • C07K5/06113Asp- or Asn-amino acid
    • C07K5/06121Asp- or Asn-amino acid the second amino acid being aromatic or cycloaliphatic
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    • C07C215/64Compounds containing amino and hydroxy groups bound to the same carbon skeleton having 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 rings other than six-membered aromatic rings being part of the carbon skeleton
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KR1020117011102A 2008-10-17 2009-10-16 페놀성 오피오이드를 약독화시켜 방출하는 약제학적 조성물 Withdrawn KR20110081852A (ko)

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US10640008P 2008-10-17 2008-10-17
US61/106,400 2008-10-17

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US (2) US8802681B2 (https=)
EP (1) EP2349241B1 (https=)
JP (2) JP5706825B2 (https=)
KR (1) KR20110081852A (https=)
CN (1) CN102186467B (https=)
AU (1) AU2009305563C1 (https=)
CA (1) CA2739936C (https=)
IL (1) IL212081A (https=)
MX (1) MX2011004095A (https=)
RU (1) RU2562583C2 (https=)
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Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8802681B2 (en) 2008-10-17 2014-08-12 Signature Therapeutics, Inc. Pharmaceutical compositions with attenuated release of phenolic opioids
US8623888B2 (en) 2009-07-15 2014-01-07 Mallinckrodt Llc 3-oxy-hydromorphone derivatives
BR112012005124B1 (pt) * 2009-09-08 2021-11-09 Signature Therapeutics, Inc. Pro-fármaco de opioide modificado por cetona, seu método de preparação, sua composição farmacêutica, sua unidade de dose, métodos e usos
US20110262359A1 (en) * 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
US20130059914A1 (en) 2010-04-21 2013-03-07 Signature Therapeutics, Inc. Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof
CA2795222A1 (en) * 2010-04-21 2011-10-27 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
WO2011133151A1 (en) * 2010-04-21 2011-10-27 Pharmacofore, Inc. Compositions comprising enzyme-cleavable phenol-modified opioid prodrugs and inhibitors thereof
US9238020B2 (en) 2010-04-21 2016-01-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
ES2584634T3 (es) * 2011-01-11 2016-09-28 Signature Therapeutics, Inc. Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente
WO2012096886A1 (en) * 2011-01-11 2012-07-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
WO2012122420A2 (en) * 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers
AU2012225337B2 (en) * 2011-03-09 2016-04-28 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
WO2016064914A1 (en) 2014-10-20 2016-04-28 Elysium Therapeutics, Inc. Diversion-resistant opioid formulations
US11634384B2 (en) 2014-11-25 2023-04-25 Concentric Analgesics, Inc. Prodrugs of phenolic TRPV1 agonists
US10335406B2 (en) * 2015-10-01 2019-07-02 Elysium Therapeutics, Inc. Opioid compositions resistant to overdose and abuse
JP2018534269A (ja) 2015-10-01 2018-11-22 エリージウム セラピューティクス, インコーポレイテッド 過剰摂取および乱用に抵抗性のポリサブユニットオピオイドプロドラッグ
EP3463576A4 (en) 2016-05-25 2020-01-15 Concentric Analgesics, Inc. PRODRUGS BY PHENOLIC TRPV1 AGONISTS IN COMBINATION WITH LOCAL ANESTHETIC AND VASOCONSTRICTORS FOR IMPROVED LOCAL ANESTHESIA
EP3595663A4 (en) * 2017-03-17 2021-01-13 Elysium Therapeutics, Inc. MULTIPLE SUBUNITY OPIOID PRODRUGS WITH RESISTANCE TO OVERDOSE AND ABUSE
US10717712B2 (en) 2018-07-27 2020-07-21 Concentric Analgesics, Inc. Pegylated prodrugs of phenolic TRPV1 agonists
US20220175699A1 (en) 2019-03-06 2022-06-09 Ensysce Biosciences, Inc. Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof
US12599578B2 (en) 2021-03-09 2026-04-14 Ensysce Biosciences Inc. Compositions comprising enzyme-cleavable prodrugs and controlled release nafamostat and methods of use thereof
MX2024003466A (es) 2021-09-29 2024-06-04 Ensysce Biosciences Inc Profarmacos de metadona escindibles por enzimas y metodos de uso de los mismos.

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU527371B2 (en) 1980-09-16 1983-03-03 Torii & Co., Ltd. Amidine
US5109118A (en) * 1989-07-06 1992-04-28 Yutaka Mizushima Modified biologically active proteins
CA2032420A1 (en) 1989-12-22 1991-06-23 Akira Okuyama Guanidinobenzene derivatives
US6692766B1 (en) 1994-06-15 2004-02-17 Yissum Research Development Company Of The Hebrew University Of Jerusalem Controlled release oral drug delivery system
US5952499A (en) * 1995-01-16 1999-09-14 Commonwealth Scientific And Industrial Research Organisation Therapeutic compound-fatty acid conjugates
US6388122B1 (en) 1996-04-10 2002-05-14 Ono Pharmaceutical Co., Ltd. Tryptase inhibitor and novel guanidino derivatives
JP4668418B2 (ja) 1998-12-15 2011-04-13 アプライド バイオシステムズ リミテッド ライアビリティー カンパニー 多種酵素アッセイ
US6849263B2 (en) * 1998-12-21 2005-02-01 Generex Pharmaceutical Incorporated Pharmaceutical compositions for buccal delivery of pain relief medications
US7060290B1 (en) 1999-02-18 2006-06-13 Supergen, Inc. Phosphocholine linked prodrug derivatives
US7060708B2 (en) 1999-03-10 2006-06-13 New River Pharmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
US20030180352A1 (en) * 1999-11-23 2003-09-25 Patel Mahesh V. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
DE60239679D1 (de) 2001-06-11 2011-05-19 Medarex Inc Methode für die ausarbeitung von cd10-aktivierten prodrug-verbindungen
US7169752B2 (en) 2003-09-30 2007-01-30 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
US7375082B2 (en) 2002-02-22 2008-05-20 Shire Llc Abuse-resistant hydrocodone compounds
US20100092562A1 (en) 2002-11-26 2010-04-15 Hollenbeck R Gary Sustained-release drug delivery compositions and methods
MXPA05012850A (es) 2003-05-29 2006-05-17 New River Pharmaceuticals Inc Compuestos de anfetamina resistentes al abuso.
EP1928881A2 (en) 2005-08-19 2008-06-11 Pharmacofore, Inc. Prodrugs of active agents
CA2620202C (en) * 2005-08-26 2016-10-04 The Board Of Trustees Of The Leland Stanford Junior University Therapy procedure for drug delivery for trigeminal pain
CN101309917B (zh) 2005-10-06 2013-09-11 奥斯拜客斯制药有限公司 具有增强治疗性质的胃h+,k+-atp酶氘代抑制剂
TWI403493B (zh) 2005-12-05 2013-08-01 Xenoport Inc 左旋多巴前藥的甲磺酸鹽,其組成物,及其用途
WO2007120864A2 (en) 2006-04-14 2007-10-25 Shire Llc Compositions and methods for enhancing analgesic potency of covalently bound compounds, attenuating its adverse side effects, and preventing their abuse
CA2653741C (en) * 2006-05-26 2015-07-07 Thomas E. Jenkins Controlled release of phenolic opioids
TWI401237B (zh) 2006-07-24 2013-07-11 3-〔(1r,2r)-3-(二甲基氨基)-1-乙基-2-甲基丙基〕酚之製備
US20110105381A2 (en) 2007-02-16 2011-05-05 Pharmacofore, Inc. Prodrugs of Peripheral Phenolic Opioid Antagonists
US20120142718A1 (en) 2007-02-16 2012-06-07 Jenkins Thomas E N-17-Alkylated Prodrugs of Opioids
CN102908339A (zh) 2007-11-23 2013-02-06 格吕伦塔尔有限公司 他喷他多组合物
US9023860B2 (en) 2007-11-26 2015-05-05 Signature Therapeutics, Inc. Pro-drugs for controlled release of biologically active compounds
US20090186832A1 (en) 2008-01-18 2009-07-23 Shire Llc Amino acid peptide pro-drugs of phenolic analgesics and uses thereof
WO2009103004A1 (en) 2008-02-14 2009-08-20 Alkermes, Inc. Selective opioid compounds
US8802681B2 (en) 2008-10-17 2014-08-12 Signature Therapeutics, Inc. Pharmaceutical compositions with attenuated release of phenolic opioids
WO2010100477A2 (en) 2009-03-03 2010-09-10 Shire Llc Amino acid and peptide carbamate prodrugs of tapentadol and uses thereof
EP2413937A1 (en) 2009-04-02 2012-02-08 Shire LLC Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof
AU2010272233A1 (en) 2009-07-17 2012-02-09 Shire Llc Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof
US20130079364A1 (en) 2010-04-21 2013-03-28 Signature Therapeutics, Inc. Peripheral Opioid Agonists and Peripheral Opioid Antagonists

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