JP2013503862A - 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物 - Google Patents

酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物 Download PDF

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JP2013503862A
JP2013503862A JP2012527871A JP2012527871A JP2013503862A JP 2013503862 A JP2013503862 A JP 2013503862A JP 2012527871 A JP2012527871 A JP 2012527871A JP 2012527871 A JP2012527871 A JP 2012527871A JP 2013503862 A JP2013503862 A JP 2013503862A
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substituted
alkyl
aryl
hydrogen
ketone
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JP2013503862A5 (enExample
Inventor
イー． ジェンキンス，トーマス
オー． フスフェルド，クレイグ
ディー． セローギー，ジュリー
ダブリュー． レイ，ジョナサン
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Signature Therapeutics Inc
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Signature Therapeutics Inc
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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (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)
  • Hydrogenated Pyridines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Plant Substances (AREA)
JP2012527871A 2009-09-08 2010-04-21 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物 Pending JP2013503862A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US24061109P 2009-09-08 2009-09-08
US61/240,611 2009-09-08
US28814809P 2009-12-18 2009-12-18
US61/288,148 2009-12-18
PCT/US2010/031956 WO2011031350A1 (en) 2009-09-08 2010-04-21 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Related Child Applications (1)

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JP2015190867A Division JP2016041698A (ja) 2009-09-08 2015-09-29 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物

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JP2013503862A true JP2013503862A (ja) 2013-02-04
JP2013503862A5 JP2013503862A5 (enExample) 2013-06-06

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JP2012527871A Pending JP2013503862A (ja) 2009-09-08 2010-04-21 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物
JP2015190867A Pending JP2016041698A (ja) 2009-09-08 2015-09-29 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物
JP2018100108A Active JP6778234B2 (ja) 2009-09-08 2018-05-25 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物

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JP2015190867A Pending JP2016041698A (ja) 2009-09-08 2015-09-29 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物
JP2018100108A Active JP6778234B2 (ja) 2009-09-08 2018-05-25 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物

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US (2) US9493477B2 (enExample)
EP (1) EP2475429B1 (enExample)
JP (3) JP2013503862A (enExample)
CN (1) CN102695545B (enExample)
AU (1) AU2010293028B2 (enExample)
BR (1) BR112012005124B1 (enExample)
CA (1) CA2773340C (enExample)
IL (1) IL218498A (enExample)
MX (1) MX348262B (enExample)
PH (1) PH12012500485A1 (enExample)
RU (1) RU2600736C2 (enExample)
SG (1) SG179026A1 (enExample)
WO (1) WO2011031350A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014502972A (ja) * 2011-01-11 2014-02-06 シグネーチャー セラピューティクス，インク． 酵素切断可能なオキシコドンプロドラッグを含んでなる組成物
JP2021504351A (ja) * 2017-11-24 2021-02-15 ビョンディス・ビー．ブイ．Ｂｙｏｎｄｉｓ Ｂ．Ｖ． リンカー薬物化合物ｖｃ−ｓｅｃｏ−ＤＵＢＡ製造のための改善された方法
JP2021532183A (ja) * 2018-07-27 2021-11-25 コンセントリック アナルジェジクス，インク． フェノール性ｔｒｐｖ１アゴニストのｐｅｇ化プロドラッグ
JP2024508946A (ja) * 2021-03-09 2024-02-28 エンサイス バイオサイエンシズ インコーポレーテッド 酵素切断可能なプロドラッグと制御放出ナファモスタットとを含む組成物及びその使用方法

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9493477B2 (en) * 2009-09-08 2016-11-15 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
CA2795222A1 (en) * 2010-04-21 2011-10-27 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
WO2011133348A1 (en) 2010-04-21 2011-10-27 Pharmacofore, Inc. Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof
WO2011141490A1 (en) 2010-05-10 2011-11-17 Euro-Celtique S.A. Combination of active loaded granules with additional actives
NZ603173A (en) 2010-05-10 2014-10-31 Euro Celtique Sa Manufacturing of active-free granules and tablets comprising the same
KR20130030260A (ko) 2010-05-10 2013-03-26 유로-셀티큐 에스.에이. 히드로모르폰 및 날록손을 포함하는 제약 조성물
AU2012225337B2 (en) 2011-03-09 2016-04-28 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
WO2012122420A2 (en) 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers
JP5977355B2 (ja) * 2011-09-29 2016-08-24 エコール ノルマル シュペリウール ドゥ リヨン ペプチダーゼの蛍光発生基質
HK1197191A1 (en) 2011-10-26 2015-01-09 Kempharm, Inc. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof
EP3068397A1 (en) 2013-11-13 2016-09-21 Euro-Celtique S.A. Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome
CN112043835B (zh) * 2013-12-06 2022-10-21 韩捷 用于含氮和羟基的药物的生物可逆引入基团
KR20170094251A (ko) 2014-12-02 2017-08-17 켐팜 인코포레이티드 옥시모르폰의 벤조산, 벤조산 유도체 및 헤테로아릴 카르복실산 콘쥬게이트, 이의 전구 약물, 제조 방법 및 용도
WO2020012245A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Thienothiophene-naltrexone prodrugs for long-acting injectable compositions
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited Naphthylenyl compounds for long-acting injectable compositions and related methods
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds for long-acting injectable compositions and related methods
CN113624665A (zh) * 2021-07-30 2021-11-09 中国药科大学 一种抗肿瘤候选化合物在治疗结直肠癌药物中的应用及测定方法
CA3230025A1 (en) 2021-09-29 2023-04-06 Lynn Kirkpatrick Enzyme-cleavable methadone prodrugs and methods of use thereof

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050176644A1 (en) * 2003-09-30 2005-08-11 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
JP2007507520A (ja) * 2003-09-30 2007-03-29 ニュー リバー ファーマシューティカルズ インコーポレイテッド 過剰摂取又は乱用を防止するための薬学組成物
WO2007120648A2 (en) * 2006-04-10 2007-10-25 Shire Llc Mono and di-substituted oxycodone compounds and compositions
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
WO2007140272A2 (en) * 2006-05-26 2007-12-06 Pharmacofore, Inc. Controlled release of phenolic opioids
US20090137618A1 (en) * 2007-11-26 2009-05-28 Jenkins Thomas E Pro-drugs for controlled release of biologically active compounds
JP2012509846A (ja) * 2008-10-17 2012-04-26 ファーマコフォア，インク． フェノール性オピオイドの放出が減弱された医薬組成物
JP2013525348A (ja) * 2010-04-21 2013-06-20 シグネーチャー セラピューティクス，インク． 酵素切断可能なオピオイドプロドラッグとそのインヒビターとを含んでなる組成物

Family Cites Families (37)

* 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
WO1997037969A1 (en) 1996-04-10 1997-10-16 Ono Pharmaceutical Co., Ltd. Tryptase inhibitor and novel guanidino derivatives
CA2353872C (en) 1998-12-15 2011-05-03 Applied Biosystems, Llc Multiple enzyme assays
ATE267586T1 (de) * 1999-02-18 2004-06-15 Supergen Inc An phosphocholin gebundene prodrug-derivate
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
US6673574B2 (en) 2000-11-30 2004-01-06 Unigene Laboratories Inc. Oral delivery of peptides using enzyme-cleavable membrane translocators
US6897034B2 (en) * 2001-06-11 2005-05-24 Medarex, Inc. CD10-activated prodrug compounds
US7375082B2 (en) * 2002-02-22 2008-05-20 Shire Llc Abuse-resistant hydrocodone compounds
RU2215741C1 (ru) * 2002-11-05 2003-11-10 Открытое Акционерное Общество "Международная Научно-Технологическая Корпорация" Сложные эфиры n-замещенных 14-гидроксиморфинанов и способ их получения
US20100092562A1 (en) 2002-11-26 2010-04-15 Hollenbeck R Gary Sustained-release drug delivery compositions and methods
KR101159477B1 (ko) 2003-05-29 2012-07-02 샤이어 엘엘씨 남용 방지성 암페타민 화합물
AU2004286239A1 (en) 2003-10-24 2005-05-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
FR2881363B1 (fr) * 2005-02-02 2008-03-14 Commissariat Energie Atomique Dispositif d'analyses biologiques avec detecteur integre
WO2007022535A2 (en) * 2005-08-19 2007-02-22 Pharmacofore, Inc. Prodrugs of active agents
WO2007025286A2 (en) 2005-08-26 2007-03-01 The Board Of Trustees Of The Leland Stanford Junior University Therapy procedure for drug delivery for trigeminal pain
US7598273B2 (en) 2005-10-06 2009-10-06 Auspex Pharmaceuticals, Inc Inhibitors of the gastric H+, K+-ATPase with enhanced therapeutic properties
EP1959948B1 (en) 2005-12-05 2012-07-18 XenoPort, Inc. Levodopa prodrug mesylate, compositions thereof, and uses thereof
US20120142718A1 (en) 2007-02-16 2012-06-07 Jenkins Thomas E N-17-Alkylated Prodrugs of Opioids
US20110105381A2 (en) 2007-02-16 2011-05-05 Pharmacofore, Inc. Prodrugs of Peripheral Phenolic Opioid Antagonists
WO2009080030A1 (en) 2007-12-21 2009-07-02 Lifecycle Pharma A/S Treatment of autoimmune hepatitis with a once daily oral dosage form comprising tacrolimus
WO2009092071A2 (en) * 2008-01-18 2009-07-23 Shire Llc Amino acid and peptide pro-drugs of phenolic analgesics and uses thereof
EP2252150B1 (en) * 2008-02-14 2018-04-11 Alkermes, Inc. Selective opioid compounds
EP2300031B1 (en) 2008-05-05 2017-09-20 Oramed Ltd. Methods and compositions for oral administration of exenatide
KR20110134510A (ko) 2009-04-02 2011-12-14 샤이어 엘엘씨 오피오이드의 신규한 디카르복실산 연결 아미노산 및 펩티드 프로드러그와 그 용도
WO2011007247A1 (en) 2009-07-17 2011-01-20 Llc Shire Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof
US9493477B2 (en) * 2009-09-08 2016-11-15 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
US20130079364A1 (en) 2010-04-21 2013-03-28 Signature Therapeutics, Inc. Peripheral Opioid Agonists and Peripheral Opioid Antagonists
US20110262360A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions Comprising Enzyme-Cleavable Phenol-Modified 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
US8497237B2 (en) * 2011-01-11 2013-07-30 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
WO2012096887A2 (en) * 2011-01-11 2012-07-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
AU2012225337B2 (en) * 2011-03-09 2016-04-28 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
WO2012122420A2 (en) * 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050176644A1 (en) * 2003-09-30 2005-08-11 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
JP2007507520A (ja) * 2003-09-30 2007-03-29 ニュー リバー ファーマシューティカルズ インコーポレイテッド 過剰摂取又は乱用を防止するための薬学組成物
WO2007120648A2 (en) * 2006-04-10 2007-10-25 Shire Llc Mono and di-substituted oxycodone compounds and compositions
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
WO2007140272A2 (en) * 2006-05-26 2007-12-06 Pharmacofore, Inc. Controlled release of phenolic opioids
US20090137618A1 (en) * 2007-11-26 2009-05-28 Jenkins Thomas E Pro-drugs for controlled release of biologically active compounds
JP2012509846A (ja) * 2008-10-17 2012-04-26 ファーマコフォア，インク． フェノール性オピオイドの放出が減弱された医薬組成物
JP2013525348A (ja) * 2010-04-21 2013-06-20 シグネーチャー セラピューティクス，インク． 酵素切断可能なオピオイドプロドラッグとそのインヒビターとを含んでなる組成物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JPN6014017363; Ｂｉｏｏｒｇａｎｉｃ　Ｃｈｅｍｉｓｔｒｙ ３０, 2002, ｐ．２８５-３０１ *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014502972A (ja) * 2011-01-11 2014-02-06 シグネーチャー セラピューティクス，インク． 酵素切断可能なオキシコドンプロドラッグを含んでなる組成物
JP2021504351A (ja) * 2017-11-24 2021-02-15 ビョンディス・ビー．ブイ．Ｂｙｏｎｄｉｓ Ｂ．Ｖ． リンカー薬物化合物ｖｃ−ｓｅｃｏ−ＤＵＢＡ製造のための改善された方法
JP7279042B2 (ja) 2017-11-24 2023-05-22 ビョンディス・ビー．ブイ． リンカー薬物化合物ｖｃ－ｓｅｃｏ－ＤＵＢＡ製造のための改善された方法
JP2021532183A (ja) * 2018-07-27 2021-11-25 コンセントリック アナルジェジクス，インク． フェノール性ｔｒｐｖ１アゴニストのｐｅｇ化プロドラッグ
JP2024508946A (ja) * 2021-03-09 2024-02-28 エンサイス バイオサイエンシズ インコーポレーテッド 酵素切断可能なプロドラッグと制御放出ナファモスタットとを含む組成物及びその使用方法

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