AU2012205733B2 - Compositions comprising enzyme-cleavable oxycodone prodrug - Google Patents

Compositions comprising enzyme-cleavable oxycodone prodrug Download PDF

Info

Publication number
AU2012205733B2
AU2012205733B2 AU2012205733A AU2012205733A AU2012205733B2 AU 2012205733 B2 AU2012205733 B2 AU 2012205733B2 AU 2012205733 A AU2012205733 A AU 2012205733A AU 2012205733 A AU2012205733 A AU 2012205733A AU 2012205733 B2 AU2012205733 B2 AU 2012205733B2
Authority
AU
Australia
Prior art keywords
compound
prodrug
oxycodone
trypsin
dose
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
AU2012205733A
Other languages
English (en)
Other versions
AU2012205733A1 (en
Inventor
Craig O. Husfeld
Thomas E. Jenkins
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 AU2012205733A1 publication Critical patent/AU2012205733A1/en
Application granted granted Critical
Publication of AU2012205733B2 publication Critical patent/AU2012205733B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
    • 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
    • A61K31/435—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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Wood Science & Technology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Psychiatry (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)
AU2012205733A 2011-01-11 2012-01-09 Compositions comprising enzyme-cleavable oxycodone prodrug Active AU2012205733B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161431781P 2011-01-11 2011-01-11
US61/431,781 2011-01-11
PCT/US2012/020649 WO2012096887A2 (en) 2011-01-11 2012-01-09 Compositions comprising enzyme-cleavable oxycodone prodrug

Publications (2)

Publication Number Publication Date
AU2012205733A1 AU2012205733A1 (en) 2013-05-09
AU2012205733B2 true AU2012205733B2 (en) 2015-10-08

Family

ID=46455749

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012205733A Active AU2012205733B2 (en) 2011-01-11 2012-01-09 Compositions comprising enzyme-cleavable oxycodone prodrug

Country Status (13)

Country Link
US (3) US8569228B2 (OSRAM)
EP (1) EP2663187B1 (OSRAM)
JP (1) JP6016810B2 (OSRAM)
CN (1) CN103384472B (OSRAM)
AU (1) AU2012205733B2 (OSRAM)
BR (1) BR112013017296B1 (OSRAM)
CA (1) CA2814763C (OSRAM)
DK (1) DK2663187T3 (OSRAM)
ES (1) ES2584634T3 (OSRAM)
IL (1) IL225904B (OSRAM)
RU (1) RU2609412C2 (OSRAM)
TW (1) TWI526209B (OSRAM)
WO (1) WO2012096887A2 (OSRAM)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2569958C (en) 2004-06-12 2016-03-22 Jane C. Hirsh Abuse-deterrent drug formulations
UA102916C2 (uk) 2009-07-02 2013-08-27 Кемфарм, Інк. Композиція на основі кон'югату гідрокодону з бензойною кислотою, похідними бензойної кислоти або гетероарилкарбоновою кислотою, проліки, спосіб лікування від зловживань
JP2013503862A (ja) 2009-09-08 2013-02-04 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
US10668060B2 (en) 2009-12-10 2020-06-02 Collegium Pharmaceutical, Inc. Tamper-resistant pharmaceutical compositions of opioids and other drugs
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
US20130059914A1 (en) 2010-04-21 2013-03-07 Signature Therapeutics, Inc. Compositions Comprising Enzyme-Cleavable Amphetamine 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
WO2012096887A2 (en) * 2011-01-11 2012-07-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
BR112013022946A2 (pt) 2011-03-09 2017-07-18 Signature Therapeutics Inc pró-fármacos de agentes ativos com ligantes heterocíclocos
US8685916B2 (en) 2011-03-09 2014-04-01 Signature Therapeutics, Inc. Opioid prodrugs with heterocyclic linkers
CN105934257B (zh) 2013-12-06 2020-10-09 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
WO2016086113A1 (en) 2014-11-25 2016-06-02 Kempharm, Inc. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone
AU2016332071B2 (en) * 2015-10-01 2019-04-18 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
EP3210630A1 (en) 2016-02-29 2017-08-30 G.L. Pharma GmbH Abuse-deterrent pharmaceutical compositions
JP2019516773A (ja) 2016-05-25 2019-06-20 コンセントリック アナルジジックス，インク． 改善された局所麻酔のための局所麻酔薬及び血管収縮薬と組み合わせたフェノールｔｒｐｖ１アゴニストのプロドラッグ
WO2017222575A1 (en) 2016-06-23 2017-12-28 Collegium Pharmaceutical, Inc. Process of making more stable abuse-deterrent oral formulations
WO2018118902A1 (en) 2016-12-19 2018-06-28 The Regents Of The University Of California Dual-enzyme responsive peptides
EP3554548A4 (en) 2016-12-19 2020-08-19 The Regents of The University of California NON-CRUSHABLE PILL FORMULATIONS
AU2018234911B2 (en) * 2017-03-17 2024-04-18 Elysium Therapeutics, Inc. Polysubunit opioid prodrugs resistant to overdose and abuse
US11666888B2 (en) 2018-02-05 2023-06-06 Bio-Rad Laboratories, Inc. Chromatography resin having an anionic exchange-hydrophobic mixed mode ligand
TW202019887A (zh) 2018-07-27 2020-06-01 美商同心止痛劑股份有限公司 酚系trpv1促效劑之聚乙二醇化前藥
MX2024003466A (es) 2021-09-29 2024-06-04 Ensysce Biosciences Inc Profarmacos de metadona escindibles por enzimas y metodos de uso de los mismos.

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010045599A1 (en) * 2008-10-17 2010-04-22 Pharmacofore, Inc. Pharmaceutical compositions with attenuated release of phenolic opioids
US20100286186A1 (en) * 2009-04-02 2010-11-11 Shire Llc Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof

Family Cites Families (56)

* 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
ES2194536T3 (es) 1998-11-13 2003-11-16 Lilly Co Eli Combinacion de duloxetina con farmacos antiinflamatorios no esteroideos.
CA2353872C (en) 1998-12-15 2011-05-03 Tropix, Inc. Multiple enzyme assays
US6849263B2 (en) 1998-12-21 2005-02-01 Generex Pharmaceutical Incorporated Pharmaceutical compositions for buccal delivery of pain relief medications
AU3000800A (en) 1999-02-18 2000-09-04 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
KR100889069B1 (ko) * 1999-10-29 2009-03-17 유로-셀티크 소시에떼 아노뉨 서방성 하이드로코돈 제형
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
DE60239679D1 (de) 2001-06-11 2011-05-19 Medarex Inc Methode für die ausarbeitung von cd10-aktivierten prodrug-verbindungen
US7375082B2 (en) 2002-02-22 2008-05-20 Shire Llc Abuse-resistant hydrocodone compounds
US7169752B2 (en) 2003-09-30 2007-01-30 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
IL163667A0 (en) 2002-02-22 2005-12-18 New River Pharmaceuticals Inc Novel sustained release pharmaceutical compounds to preventabuse 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
ATE454169T1 (de) 2003-03-13 2010-01-15 Controlled Chemicals Inc Oxycodon- konjugate mit niedrigerem missbrauch- potential und ausgedehnter tätigkeitsdauer
BRPI0410792B8 (pt) 2003-05-29 2021-05-25 New River Pharmaceuticals Inc compostos de anfetamina resistentes à dependencia
NZ546226A (en) 2003-09-30 2009-03-31 Shire Llc Oxycodone conjugates for prevention of overdose or abuse
CA2543294A1 (en) 2003-10-24 2005-05-26 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
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
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
RU2429223C2 (ru) 2005-12-05 2011-09-20 Ксенопорт, Инк. Мезилатное пролекарство леводопы, его композиции и применение
CA2649360A1 (en) 2006-04-10 2007-10-25 Shire Llc Mono and di-substituted oxycodone compounds and compositions
JP2009533459A (ja) 2006-04-14 2009-09-17 シャイア エルエルシー 共有結合する化合物の鎮痛作用の増強と、有害な副作用の減衰と、前記化合物の乱用の予防とのための組成物及び方法
SG172633A1 (en) 2006-05-26 2011-07-28 Pharmacofore Inc 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
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
WO2008101202A1 (en) 2007-02-16 2008-08-21 Pharmacofore, Inc. N-17-alkylated prodrugs of opioids
US20110105381A2 (en) * 2007-02-16 2011-05-05 Pharmacofore, Inc. Prodrugs of Peripheral Phenolic Opioid Antagonists
PL2596784T3 (pl) 2007-11-23 2017-06-30 Grünenthal GmbH Kompozycje tapentadolu
US9023860B2 (en) 2007-11-26 2015-05-05 Signature Therapeutics, Inc. Pro-drugs for controlled release of biologically active compounds
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
US20090186832A1 (en) 2008-01-18 2009-07-23 Shire Llc Amino acid peptide pro-drugs of phenolic analgesics and uses thereof
AU2009214500B2 (en) 2008-02-14 2014-10-23 Alkermes, Inc. Selective opioid compounds
NZ589390A (en) 2008-05-05 2011-11-25 Oramed Ltd Methods and compositions for oral administration of exenatide
US20100227921A1 (en) 2009-03-03 2010-09-09 Shire Llc Amino acid and peptide carbamate prodrugs of tapentadol 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
JP2013503862A (ja) * 2009-09-08 2013-02-04 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
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
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
US20110262360A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof
US20130059914A1 (en) 2010-04-21 2013-03-07 Signature Therapeutics, Inc. Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof
BR112012026768A2 (pt) * 2010-04-21 2015-09-29 Signature Therapeutics Inc composições compreendendo pró-farmacos de opioides cliváveis de modo enzimático e seus inibidores.
WO2011133150A1 (en) * 2010-04-21 2011-10-27 Pharmacofore, Inc. 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
WO2012096887A2 (en) 2011-01-11 2012-07-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
WO2012096886A1 (en) 2011-01-11 2012-07-19 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
BR112013022946A2 (pt) 2011-03-09 2017-07-18 Signature Therapeutics Inc pró-fármacos de agentes ativos com ligantes heterocíclocos

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010045599A1 (en) * 2008-10-17 2010-04-22 Pharmacofore, Inc. Pharmaceutical compositions with attenuated release of phenolic opioids
US20100286186A1 (en) * 2009-04-02 2010-11-11 Shire Llc Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof

Also Published As

Publication number Publication date
WO2012096887A2 (en) 2012-07-19
BR112013017296A2 (pt) 2017-09-05
TW201309297A (zh) 2013-03-01
US8962547B2 (en) 2015-02-24
RU2609412C2 (ru) 2017-02-01
US20120178772A1 (en) 2012-07-12
CA2814763C (en) 2019-05-28
US9499581B2 (en) 2016-11-22
HK1189763A1 (zh) 2014-06-20
AU2012205733A1 (en) 2013-05-09
CA2814763A1 (en) 2012-07-19
ES2584634T3 (es) 2016-09-28
CN103384472B (zh) 2016-01-20
WO2012096887A3 (en) 2012-10-04
TWI526209B (zh) 2016-03-21
EP2663187B1 (en) 2016-06-01
EP2663187A4 (en) 2014-09-10
RU2013137452A (ru) 2015-02-20
EP2663187A2 (en) 2013-11-20
DK2663187T3 (en) 2016-08-29
JP2014502972A (ja) 2014-02-06
US8569228B2 (en) 2013-10-29
JP6016810B2 (ja) 2016-10-26
US20140162935A1 (en) 2014-06-12
BR112013017296B1 (pt) 2021-02-17
IL225904B (en) 2020-03-31
CN103384472A (zh) 2013-11-06
US20150197544A1 (en) 2015-07-16

Similar Documents

Publication Publication Date Title
AU2012205733B2 (en) Compositions comprising enzyme-cleavable oxycodone prodrug
US8497237B2 (en) Compositions comprising enzyme-cleavable oxycodone prodrug
US8685916B2 (en) Opioid prodrugs with heterocyclic linkers
AU2012225337B2 (en) Active agent prodrugs with heterocyclic linkers
AU2010293028B2 (en) Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
WO2011133179A1 (en) Compositions comprising enzyme-cleavable hydromorphone prodrug
HK1189763B (en) Compositions comprising enzyme-cleavable oxycodone prodrug
HK1193976A (en) Active agent prodrugs with heterocyclic linkers
HK1193976B (en) Active agent prodrugs with heterocyclic linkers
AU2015201341A1 (en) Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
HK1172283B (en) Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)