JP6148182B2 - 複素環式リンカーを有する活性薬剤プロドラッグ - Google Patents

複素環式リンカーを有する活性薬剤プロドラッグ Download PDF

Info

Publication number
JP6148182B2
JP6148182B2 JP2013557882A JP2013557882A JP6148182B2 JP 6148182 B2 JP6148182 B2 JP 6148182B2 JP 2013557882 A JP2013557882 A JP 2013557882A JP 2013557882 A JP2013557882 A JP 2013557882A JP 6148182 B2 JP6148182 B2 JP 6148182B2
Authority
JP
Japan
Prior art keywords
substituted
alkyl
aryl
acyl
active agent
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
JP2013557882A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014518546A5 (enExample
JP2014518546A (ja
Inventor
イー． ジェンキンス，トーマス
イー． ジェンキンス，トーマス
オー． フスフェルド，クレイグ
オー． フスフェルド，クレイグ
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 JP2014518546A publication Critical patent/JP2014518546A/ja
Publication of JP2014518546A5 publication Critical patent/JP2014518546A5/ja
Application granted granted Critical
Publication of JP6148182B2 publication Critical patent/JP6148182B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Cell Biology (AREA)
  • Psychiatry (AREA)
JP2013557882A 2011-03-09 2012-03-08 複素環式リンカーを有する活性薬剤プロドラッグ Active JP6148182B2 (ja)

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 (3)

Publication Number Publication Date
JP2014518546A JP2014518546A (ja) 2014-07-31
JP2014518546A5 JP2014518546A5 (enExample) 2015-04-30
JP6148182B2 true JP6148182B2 (ja) 2017-06-14

Family

ID=46798816

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013557882A Active JP6148182B2 (ja) 2011-03-09 2012-03-08 複素環式リンカーを有する活性薬剤プロドラッグ

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 (34)

* 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
WO2011133348A1 (en) 2010-04-21 2011-10-27 Pharmacofore, 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
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
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
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
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
GB2556817B (en) 2015-10-01 2019-11-06 Elysium Therapeutics Inc Polysubunit opioid prodrugs resistant to overdose and abuse
US10335406B2 (en) 2015-10-01 2019-07-02 Elysium Therapeutics, Inc. Opioid compositions resistant to overdose and abuse
US10369292B2 (en) * 2016-01-15 2019-08-06 W. L. Gore & Associates, Inc. Syringe plunger assemblies
EP3231420A1 (en) * 2016-02-29 2017-10-18 G.L. Pharma GmbH Abuse-deterrent pharmaceutical compositions
EP3210630A1 (en) * 2016-02-29 2017-08-30 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
US10821105B2 (en) 2016-05-25 2020-11-03 Concentric Analgesics, Inc. Prodrugs of phenolic TRPV1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia
HRP20220479T1 (hr) 2016-06-01 2022-05-27 Athira Pharma, Inc. Spojevi
EP3481835A4 (en) 2016-07-05 2020-02-26 Blade Therapeutics, Inc. CALPAIN MODULATORS AND THERAPEUTIC USE THEREOF
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
WO2018118902A1 (en) 2016-12-19 2018-06-28 The Regents Of The University Of California Dual-enzyme responsive peptides
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
AU2018234911B2 (en) 2017-03-17 2024-04-18 Elysium Therapeutics, Inc. Polysubunit opioid prodrugs resistant to overdose and abuse
AU2019224127B2 (en) * 2018-02-23 2021-12-09 Rhodes Technologies Novel opioid compounds and uses thereof
CA3107433A1 (en) 2018-07-27 2020-01-30 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
JP2023505687A (ja) 2019-12-11 2023-02-10 インスピルナ，インコーポレーテッド 癌の処置方法
JP2024509872A (ja) * 2021-03-09 2024-03-05 エンサイス バイオサイエンシズ インコーポレーテッド ナファモスタットの放出調節組成物及びその使用方法
MX2023010506A (es) 2021-03-09 2023-09-20 Ensysce Biosciences Inc Composiciones que comprenden profarmacos de escision enzimatica y nafamostat de liberacion controlada y metodos de uso de estos.
CA3224494A1 (en) 2021-07-09 2023-01-12 Koen Vandyck 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
WO1997037969A1 (en) 1996-04-10 1997-10-16 Ono Pharmaceutical Co., Ltd. Tryptase inhibitor and novel guanidino derivatives
DE69905938T2 (de) 1998-11-13 2003-11-13 Eli Lilly And Co., Indianapolis Kombination von duloxetin mit nichtsteroid-entzündungshemmern für die behandlung von schmerz
CA2353872C (en) 1998-12-15 2011-05-03 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
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
WO2005032474A2 (en) 2003-09-30 2005-04-14 New River Pharmaceuticals Inc. Pharmaceutical compositions for prevention of overdose or abuse
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
US7169752B2 (en) 2003-09-30 2007-01-30 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
AU2003219863C1 (en) 2002-02-22 2009-03-05 Shire Llc Novel 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
MXPA05009757A (es) 2003-03-13 2005-12-05 Controlled Chemicals Inc Conjugados de oxicodona con menor potencial de abuso y duracion de accion extendida.
KR101159477B1 (ko) 2003-05-29 2012-07-02 샤이어 엘엘씨 남용 방지성 암페타민 화합물
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
EP2007762A2 (en) 2006-04-10 2008-12-31 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
JP5371746B2 (ja) 2006-05-26 2013-12-18 ファーマコフォア， インコーポレイテッド フェノール性オピオイドの制御放出
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
KR20090055616A (ko) 2006-09-14 2009-06-02 스타파이어 시스템즈, 인크. 고리형 유기실란의 합성 방법
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
EP2252150B1 (en) 2008-02-14 2018-04-11 Alkermes, Inc. Selective opioid compounds
CA2739936C (en) * 2008-10-17 2017-12-12 Pharmacofore, Inc. Pharmaceutical compositions with attenuated release of phenolic opioids
US20100227921A1 (en) 2009-03-03 2010-09-09 Shire Llc Amino acid and peptide carbamate prodrugs of tapentadol and uses thereof
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
WO2011133348A1 (en) 2010-04-21 2011-10-27 Pharmacofore, 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
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
US20110262359A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
US9238020B2 (en) 2010-04-21 2016-01-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
DE102010042013A1 (de) * 2010-10-06 2012-04-12 Robert Bosch Gmbh Verfahren zur Einstellung einer Temperatur eines Sensorelements
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
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

Also Published As

Publication number Publication date
CN103813800B (zh) 2017-12-19
WO2012122422A3 (en) 2014-04-24
CA2827662A1 (en) 2012-09-13
US9139612B2 (en) 2015-09-22
AU2012225337A1 (en) 2013-05-09
EP2683394A2 (en) 2014-01-15
IL228215B (en) 2019-01-31
CN103813800A (zh) 2014-05-21
JP2014518546A (ja) 2014-07-31
CA2827662C (en) 2020-07-14
RU2608305C2 (ru) 2017-01-17
US20140121152A1 (en) 2014-05-01
EP2683394A4 (en) 2015-06-03
US20160002291A1 (en) 2016-01-07
AU2012225337B2 (en) 2016-04-28
BR112013022946A2 (pt) 2017-07-18
WO2012122422A2 (en) 2012-09-13
RU2013144368A (ru) 2015-04-10
EP2683394B1 (en) 2021-01-06

Similar Documents

Publication Publication Date Title
RU2608305C2 (ru) Пролекарства действующих веществ гетероциклическими линкерами
US9095627B2 (en) Opioid prodrugs with heterocyclic linkers
JP6778234B2 (ja) 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
DK2663187T3 (en) Compositions comprising enzyme-cleavable oxycodone prodrug
US8497237B2 (en) Compositions comprising enzyme-cleavable oxycodone prodrug
JP2013525348A (ja) 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
US20110262360A1 (en) Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof
US9238020B2 (en) Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
US20120232066A1 (en) Compositions for reducing risk of adverse events caused by drug-drug interactions
JP2015199772A (ja) 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
HK1193976B (en) Active agent prodrugs with heterocyclic linkers
HK1193976A (en) Active agent prodrugs with heterocyclic linkers
HK1172283B (en) Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150309

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150309

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20151029

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20151030

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20151224

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160502

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160526

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160824

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20161025

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161125

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20170421

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20170518

R150 Certificate of patent or registration of utility model

Ref document number: 6148182

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250