CA2827662C - Active agent prodrugs with heterocyclic linkers - Google Patents

Active agent prodrugs with heterocyclic linkers Download PDF

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Publication number
CA2827662C
CA2827662C CA2827662A CA2827662A CA2827662C CA 2827662 C CA2827662 C CA 2827662C CA 2827662 A CA2827662 A CA 2827662A CA 2827662 A CA2827662 A CA 2827662A CA 2827662 C CA2827662 C CA 2827662C
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CA
Canada
Prior art keywords
substituted
alkyl
aryl
acyl
alkoxycarbonyl
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.)
Active
Application number
CA2827662A
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English (en)
French (fr)
Other versions
CA2827662A1 (en
Inventor
Thomas E. Jenkins
Craig O. Husfeld
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.)
Signature Therapeutics Inc
Original Assignee
Signature Therapeutics Inc
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 Signature Therapeutics Inc filed Critical Signature Therapeutics Inc
Publication of CA2827662A1 publication Critical patent/CA2827662A1/en
Application granted granted Critical
Publication of CA2827662C publication Critical patent/CA2827662C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C07K5/06095—Arg-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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • 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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Crystallography & Structural Chemistry (AREA)
CA2827662A 2011-03-09 2012-03-08 Active agent prodrugs with heterocyclic linkers Active CA2827662C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161451019P 2011-03-09 2011-03-09
US61/451,019 2011-03-09
US201261583523P 2012-01-05 2012-01-05
US61/583,523 2012-01-05
PCT/US2012/028367 WO2012122422A2 (en) 2011-03-09 2012-03-08 Active agent prodrugs with heterocyclic linkers

Publications (2)

Publication Number Publication Date
CA2827662A1 CA2827662A1 (en) 2012-09-13
CA2827662C true CA2827662C (en) 2020-07-14

Family

ID=46798816

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2827662A Active CA2827662C (en) 2011-03-09 2012-03-08 Active agent prodrugs with heterocyclic linkers

Country Status (10)

Country Link
US (2) US9139612B2 (enExample)
EP (1) EP2683394B1 (enExample)
JP (1) JP6148182B2 (enExample)
CN (1) CN103813800B (enExample)
AU (1) AU2012225337B2 (enExample)
BR (1) BR112013022946A2 (enExample)
CA (1) CA2827662C (enExample)
IL (1) IL228215B (enExample)
RU (1) RU2608305C2 (enExample)
WO (1) WO2012122422A2 (enExample)

Families Citing this family (33)

* 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
US20130059914A1 (en) 2010-04-21 2013-03-07 Signature Therapeutics, Inc. Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
BR112013017296B1 (pt) 2011-01-11 2021-02-17 Signature Therapeutics, Inc. composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina
JP6148182B2 (ja) 2011-03-09 2017-06-14 シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. 複素環式リンカーを有する活性薬剤プロドラッグ
US8685916B2 (en) 2011-03-09 2014-04-01 Signature Therapeutics, Inc. Opioid prodrugs with heterocyclic linkers
EP2760844B1 (fr) 2011-09-29 2018-11-21 Ecole Normale Superieure De Lyon Substrat de peptidase fluorogene
EP3077008B1 (en) 2013-12-06 2023-10-04 Jie Han Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs
US11634384B2 (en) 2014-11-25 2023-04-25 Concentric Analgesics, Inc. Prodrugs of phenolic TRPV1 agonists
US20170056352A1 (en) 2015-08-25 2017-03-02 Rgenix, Inc. PHARMACEUTICALLY ACCEPTABLE SALTS OF beta-GUANIDINOPROPIONIC ACID WITH IMPROVED PROPERTIES AND USES THEREOF
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
US10369292B2 (en) * 2016-01-15 2019-08-06 W. L. Gore & Associates, Inc. Syringe plunger assemblies
EP3210630A1 (en) * 2016-02-29 2017-08-30 G.L. Pharma GmbH Abuse-deterrent pharmaceutical compositions
EP3231420A1 (en) 2016-02-29 2017-10-18 G.L. Pharma GmbH Abuse-deterrent pharmaceutical compositions
EP3210596A1 (en) 2016-02-29 2017-08-30 G.L. Pharma GmbH Abuse-deterrent pharmaceutical composition
EP3426674A4 (en) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
CN109562281B (zh) * 2016-05-25 2021-12-17 同心镇痛药物公司 酚类trpv1激动剂的前药与局部麻醉药和血管收缩剂联合用于改善局部麻醉
HRP20220479T1 (hr) 2016-06-01 2022-05-27 Athira Pharma, Inc. Spojevi
AU2017292646A1 (en) 2016-07-05 2019-02-07 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
KR20190063473A (ko) 2016-09-28 2019-06-07 블레이드 테라퓨틱스, 인크. 칼페인 조정자 및 그 치료학적 용도
EP3555280A4 (en) * 2016-12-19 2020-09-09 The Regents of The University of California PEPTIDES SENSITIVE TO TWO ENZYMES
US11541125B2 (en) 2016-12-19 2023-01-03 The Regents Of The University Of California Noncrushable pill formulations
WO2018160178A1 (en) 2017-03-01 2018-09-07 Rgenix, Inc. Pharmaceutically acceptable salts of b-guanidinopropionic acid with improved properties and uses thereof
WO2018170465A1 (en) 2017-03-17 2018-09-20 Elysium Therapeutics, Inc. Polysubunit opioid prodrugs resistant to overdose and abuse
CA3091826A1 (en) * 2018-02-23 2019-08-29 Rhodes Technologies Novel opioid compounds and uses thereof
US10717712B2 (en) 2018-07-27 2020-07-21 Concentric Analgesics, Inc. Pegylated prodrugs of phenolic TRPV1 agonists
WO2020181000A1 (en) 2019-03-06 2020-09-10 Ensysce Biosciences, Inc. Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof
AU2020402994A1 (en) 2019-12-11 2022-06-23 Inspirna, Inc. Methods of treating cancer
KR20230175187A (ko) * 2021-03-09 2023-12-29 엔사이스 바이오사이언시즈 인크. 효소-절단가능한 전구약물 및 제어된 방출 나파모스타트를 포함하는 조성물 및 그의 사용 방법
AU2022306289A1 (en) 2021-07-09 2024-01-18 Aligos Therapeutics, Inc. Anti-viral compounds
WO2023043816A1 (en) 2021-09-17 2023-03-23 Aligos Therapeutics, Inc. Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections
CA3230025A1 (en) 2021-09-29 2023-04-06 Lynn Kirkpatrick Enzyme-cleavable methadone prodrugs and methods of use thereof

Family Cites Families (51)

* 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
US5217987A (en) 1989-10-30 1993-06-08 Berger Stephen P Dopamine uptake inhibitors in reducing substance abuse and/or craving
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
KR20000005312A (ko) 1996-04-10 2000-01-25 오노 야꾸힝 고교 가부시키가이샤 트립타아제 억제제 및 신규 구아니디노 유도체
WO2000028980A2 (en) 1998-11-13 2000-05-25 Eli Lilly And Company Combination of duloxetine with non-steroidal antiinflammatory drug for treating pain
AU781255B2 (en) 1998-12-15 2005-05-12 Applied Biosystems, Llc Multiple enzyme assays
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
US6673574B2 (en) 2000-11-30 2004-01-06 Unigene Laboratories Inc. Oral delivery of peptides using enzyme-cleavable membrane translocators
JP4541693B2 (ja) 2001-06-11 2010-09-08 メダレックス，インコーポレイティド Ｃｄ１０活性化プロドラッグ化合物
US7169752B2 (en) 2003-09-30 2007-01-30 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
EP2319540A1 (en) 2002-02-22 2011-05-11 Shire LLC Sustained release pharmaceutical compounds to prevent abuse of controlled substances
US20100092562A1 (en) 2002-11-26 2010-04-15 Hollenbeck R Gary Sustained-release drug delivery compositions and methods
EP1782834A3 (en) 2003-03-13 2007-08-01 Controlled Chemicals, Inc. Oxycodone conjugates with lower abuse potential and extended duration of action
JP2006520392A (ja) 2003-03-13 2006-09-07 コントロールド・ケミカルズ・インコーポレーテッド 薬物の乱用可能性を低下させ且つ作用持続時間を延長する化合物および方法
KR101159477B1 (ko) 2003-05-29 2012-07-02 샤이어 엘엘씨 남용 방지성 암페타민 화합물
EP1675555A4 (en) 2003-09-30 2011-03-09 Shire Llc PHARMACEUTICAL COMPOSITIONS FOR PREVENTING EXCESSIVE DOSE OR ABUSE
US8163701B2 (en) 2005-08-19 2012-04-24 Signature Therapeutics, 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
CN101365439B (zh) 2005-12-05 2012-12-26 克塞诺波特公司 左旋多巴前体药物甲磺酸盐、其组合物及其用途
EP2007762A2 (en) 2006-04-10 2008-12-31 Shire LLC Mono and di-substituted oxycodone compounds and compositions
CA2648659A1 (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
KR20090031519A (ko) 2006-05-26 2009-03-26 파마코포어, 인크. 페놀계 오피오이드의 제어 방출
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
JP2010503700A (ja) 2006-09-14 2010-02-04 スターファイアー システムズ， インコーポレイテッド 環式有機シランの合成方法
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
EP2219633A2 (en) 2007-11-23 2010-08-25 Nectid, Inc. Tapentadol compositions
US9023860B2 (en) 2007-11-26 2015-05-05 Signature Therapeutics, Inc. Pro-drugs for controlled release of biologically active compounds
JP2011512360A (ja) 2008-02-14 2011-04-21 アルカーメス，インコーポレイテッド 選択的オピオイド化合物
MX2011004095A (es) 2008-10-17 2011-07-28 Pharmacofore Inc Composiciones farmaceuticas con liberacion atenuada de opioides fenolicos.
US20100227921A1 (en) 2009-03-03 2010-09-09 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
JP2013527124A (ja) * 2009-07-17 2013-06-27 シャイア エルエルシー オピオイドの新規カルバマートアミノ酸およびペプチドプロドラッグならびにその使用
US9493477B2 (en) 2009-09-08 2016-11-15 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
US20110262360A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof
WO2011133178A1 (en) 2010-04-21 2011-10-27 Pharmacofore, Inc Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
US20110262359A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
EP2560491A1 (en) 2010-04-21 2013-02-27 Signature Therapeutics, Inc. Peripheral opioid agonists and peripheral opioid antagonists
US20130059914A1 (en) 2010-04-21 2013-03-07 Signature Therapeutics, Inc. Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
DE102010042013A1 (de) * 2010-10-06 2012-04-12 Robert Bosch Gmbh Verfahren zur Einstellung einer Temperatur eines Sensorelements
BR112013017296B1 (pt) 2011-01-11 2021-02-17 Signature Therapeutics, Inc. composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina
US8497237B2 (en) 2011-01-11 2013-07-30 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
US8685916B2 (en) * 2011-03-09 2014-04-01 Signature Therapeutics, Inc. Opioid prodrugs with heterocyclic linkers
JP6148182B2 (ja) 2011-03-09 2017-06-14 シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. 複素環式リンカーを有する活性薬剤プロドラッグ

Also Published As

Publication number Publication date
WO2012122422A3 (en) 2014-04-24
US9139612B2 (en) 2015-09-22
RU2013144368A (ru) 2015-04-10
WO2012122422A2 (en) 2012-09-13
CA2827662A1 (en) 2012-09-13
EP2683394B1 (en) 2021-01-06
CN103813800A (zh) 2014-05-21
JP6148182B2 (ja) 2017-06-14
CN103813800B (zh) 2017-12-19
AU2012225337A1 (en) 2013-05-09
AU2012225337B2 (en) 2016-04-28
EP2683394A4 (en) 2015-06-03
BR112013022946A2 (pt) 2017-07-18
EP2683394A2 (en) 2014-01-15
IL228215B (en) 2019-01-31
US20160002291A1 (en) 2016-01-07
RU2608305C2 (ru) 2017-01-17
JP2014518546A (ja) 2014-07-31
US20140121152A1 (en) 2014-05-01

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