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

Compositions comprising enzyme-cleavable oxycodone prodrug Download PDF

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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
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AU
Australia
Prior art keywords
compound
prodrug
oxycodone
trypsin
dose
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AU2012205733A
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AU2012205733A1 (en
Inventor
Craig O. Husfeld
Thomas E. Jenkins
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Signature Therapeutics Inc
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Signature Therapeutics Inc
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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
    • C07K5/08—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

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  • 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)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (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 (enExample)
EP (1) EP2663187B1 (enExample)
JP (1) JP6016810B2 (enExample)
CN (1) CN103384472B (enExample)
AU (1) AU2012205733B2 (enExample)
BR (1) BR112013017296B1 (enExample)
CA (1) CA2814763C (enExample)
DK (1) DK2663187T3 (enExample)
ES (1) ES2584634T3 (enExample)
IL (1) IL225904B (enExample)
RU (1) RU2609412C2 (enExample)
TW (1) TWI526209B (enExample)
WO (1) WO2012096887A2 (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1765292T3 (en) 2004-06-12 2018-01-02 Collegium Pharmaceutical Inc ABUSE PREVENTIONAL PHARMACEUTICAL 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
US20110262359A1 (en) * 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
ES2710617T3 (es) 2010-04-21 2019-04-26 Signature Therapeutics Inc Composiciones que comprenden profármacos de anfetamina escindibles enzimáticamente e inhibidores de los mismos
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
ES2584634T3 (es) 2011-01-11 2016-09-28 Signature Therapeutics, Inc. Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente
EP2683394B1 (en) 2011-03-09 2021-01-06 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
US8685916B2 (en) 2011-03-09 2014-04-01 Signature Therapeutics, Inc. Opioid prodrugs with heterocyclic linkers
AU2014359894B2 (en) 2013-12-06 2020-09-17 Baikang (Suzhou) Co., Ltd 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
WO2016086113A1 (en) * 2014-11-25 2016-06-02 Kempharm, Inc. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone
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
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
EP3463576A4 (en) 2016-05-25 2020-01-15 Concentric Analgesics, Inc. MEDICINAL PRODUCTS BASED ON PHENOLIC TRPV1 AGONISTS IN ASSOCIATION WITH LOCAL ANESTHETICS AND VASOCONSTRUCTS TO IMPROVE LOCAL ANESTHESIA
US9737530B1 (en) 2016-06-23 2017-08-22 Collegium Pharmaceutical, Inc. Process of making stable abuse-deterrent oral formulations
US11879019B2 (en) 2016-12-19 2024-01-23 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
WO2018170465A1 (en) * 2017-03-17 2018-09-20 Elysium Therapeutics, Inc. Polysubunit opioid prodrugs resistant to overdose and abuse
CN111683976B (zh) 2018-02-05 2022-11-18 生物辐射实验室股份有限公司 具有阴离子交换-疏水混合模式配体的色谱树脂
WO2020023794A1 (en) 2018-07-27 2020-01-30 Concentric Analgesics, Inc. Pegylated prodrugs of phenolic trpv1 agonists
CA3230025A1 (en) 2021-09-29 2023-04-06 Lynn Kirkpatrick Enzyme-cleavable methadone prodrugs and methods of use thereof

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
KR20000005312A (ko) 1996-04-10 2000-01-25 오노 야꾸힝 고교 가부시키가이샤 트립타아제 억제제 및 신규 구아니디노 유도체
CA2350531A1 (en) 1998-11-13 2000-05-25 Smriti Iyengar Method for treating pain
US6586196B1 (en) 1998-12-15 2003-07-01 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
EP1161226B1 (en) 1999-02-18 2004-05-26 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
EP1623703B1 (en) * 1999-10-29 2011-10-05 Euro-Celtique S.A. Controlled release hydrocodone formulations
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
US7169752B2 (en) 2003-09-30 2007-01-30 New River Pharmaceuticals Inc. Compounds and compositions for prevention of overdose of oxycodone
KR100822498B1 (ko) 2002-02-22 2008-04-16 샤이어 엘엘씨 규제된 물질의 남용을 방지하기 위한 새로운 서방성 약학화합물
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.
NZ544162A (en) 2003-05-29 2008-09-26 Shire Llc Abuse resistant amphetamine compounds
NZ546226A (en) 2003-09-30 2009-03-31 Shire Llc Oxycodone conjugates for prevention of overdose or abuse
US7273717B2 (en) 2003-10-24 2007-09-25 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds with GS-9005 ester hydrolase B
EP1928881A2 (en) * 2005-08-19 2008-06-11 Pharmacofore, Inc. Prodrugs of active agents
AU2006282799B2 (en) 2005-08-26 2012-11-29 Healthpartners Research & Education Methods for treatment of headaches by administration of oxytocin
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
PT1959948E (pt) 2005-12-05 2012-09-12 Xenoport Inc Mesilato de pró-fármaco de levodopa, suas composições e suas utilizações
JP2009533443A (ja) 2006-04-10 2009-09-17 シャイア エルエルシー 一置換及び二置換のオキシコドン化合物及び組成物
AU2007238625A1 (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
ES2456674T3 (es) 2006-05-26 2014-04-23 Signature Therapeutics, Inc. Liberación controlada de opioides fenólicos
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
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
NZ586361A (en) 2007-11-23 2012-09-28 Gruenenthal Chemie Tapentadol compositions
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
US20090192095A1 (en) 2008-01-18 2009-07-30 Shire Llc Amino acid and peptide prodrugs of opioid analgesics with reduced gi side-effects
AU2009214500B2 (en) 2008-02-14 2014-10-23 Alkermes, Inc. Selective opioid compounds
CN105903005A (zh) 2008-05-05 2016-08-31 奥拉姆德有限公司 用于口服给予艾塞那肽的方法和组合物
US20100227921A1 (en) 2009-03-03 2010-09-09 Shire Llc Amino acid and peptide carbamate prodrugs of tapentadol and uses thereof
US20120270847A1 (en) 2009-07-17 2012-10-25 Shire Llc Novel carbamate amino acid and peptide prodrugs of opiates and uses thereof
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
AU2010351605C1 (en) * 2010-04-21 2015-08-06 Signature Therapeutics, Inc. 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
US9238020B2 (en) 2010-04-21 2016-01-19 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
US20130079364A1 (en) * 2010-04-21 2013-03-28 Signature Therapeutics, Inc. Peripheral Opioid Agonists and Peripheral Opioid Antagonists
EP2560490A1 (en) * 2010-04-21 2013-02-27 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable prodrugs of active agents 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
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
ES2710617T3 (es) 2010-04-21 2019-04-26 Signature Therapeutics Inc Composiciones que comprenden profármacos de anfetamina escindibles enzimáticamente e inhibidores de los mismos
US8497237B2 (en) 2011-01-11 2013-07-30 Signature Therapeutics, Inc. Compositions comprising enzyme-cleavable oxycodone prodrug
ES2584634T3 (es) * 2011-01-11 2016-09-28 Signature Therapeutics, Inc. Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente
EP2683394B1 (en) 2011-03-09 2021-01-06 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
US8685916B2 (en) 2011-03-09 2014-04-01 Signature Therapeutics, Inc. Opioid prodrugs with heterocyclic linkers

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

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