AU2012225337B2 - Active agent prodrugs with heterocyclic linkers - Google Patents

Active agent prodrugs with heterocyclic linkers Download PDF

Info

Publication number
AU2012225337B2
AU2012225337B2 AU2012225337A AU2012225337A AU2012225337B2 AU 2012225337 B2 AU2012225337 B2 AU 2012225337B2 AU 2012225337 A AU2012225337 A AU 2012225337A AU 2012225337 A AU2012225337 A AU 2012225337A AU 2012225337 B2 AU2012225337 B2 AU 2012225337B2
Authority
AU
Australia
Prior art keywords
substituted
alkyl
active agent
aryl
ring
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
AU2012225337A
Other languages
English (en)
Other versions
AU2012225337A1 (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 AU2012225337A1 publication Critical patent/AU2012225337A1/en
Application granted granted Critical
Publication of AU2012225337B2 publication Critical patent/AU2012225337B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • C07K5/06095Arg-amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/94Chemical 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Food Science & Technology (AREA)
  • Analytical Chemistry (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • General Physics & Mathematics (AREA)
  • Physics & Mathematics (AREA)
  • Crystallography & Structural Chemistry (AREA)
AU2012225337A 2011-03-09 2012-03-08 Active agent prodrugs with heterocyclic linkers Active AU2012225337B2 (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
AU2012225337A1 AU2012225337A1 (en) 2013-05-09
AU2012225337B2 true AU2012225337B2 (en) 2016-04-28

Family

ID=46798816

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012225337A Active AU2012225337B2 (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
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
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
CN103384472B (zh) 2011-01-11 2016-01-20 特色疗法股份有限公司 包含酶可裂解的羟考酮药物前体的组合物
WO2012122420A2 (en) 2011-03-09 2012-09-13 Pharmacofore, 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
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
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
AU2016332071B2 (en) 2015-10-01 2019-04-18 Elysium Therapeutics, Inc. Polysubunit opioid prodrugs resistant to overdose and abuse
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
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
EP4067368A1 (en) 2016-06-01 2022-10-05 Athira Pharma, Inc. Compounds
AU2017292646A1 (en) 2016-07-05 2019-02-07 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
US11879019B2 (en) 2016-12-19 2024-01-23 The Regents Of The University Of California Dual-enzyme responsive peptides
WO2018118903A1 (en) * 2016-12-19 2018-06-28 The Regents Of The University Of California Noncrushable pill formulatiions
WO2018160178A1 (en) 2017-03-01 2018-09-07 Rgenix, Inc. Pharmaceutically acceptable salts of b-guanidinopropionic acid with improved properties and uses thereof
CA3056239C (en) 2017-03-17 2023-09-12 Elysium Therapeutics, Inc. Polysubunit opioid prodrugs resistant to overdose and abuse
MX2020008706A (es) * 2018-02-23 2020-09-25 Rhodes Tech Nuevos compuestos de opioides y sus usos.
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
WO2020181000A1 (en) 2019-03-06 2020-09-10 Ensysce Biosciences, Inc. Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof
WO2021119316A1 (en) 2019-12-11 2021-06-17 Rgenix, Inc. Methods of treating cancer
JP2024508946A (ja) * 2021-03-09 2024-02-28 エンサイス バイオサイエンシズ インコーポレーテッド 酵素切断可能なプロドラッグと制御放出ナファモスタットとを含む組成物及びその使用方法
US11851422B2 (en) 2021-07-09 2023-12-26 Aligos Therapeutics, Inc. Anti-viral compounds
US12065428B2 (en) 2021-09-17 2024-08-20 Aligos Therapeutics, Inc. Anti-viral compounds
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012045599A1 (de) * 2010-10-06 2012-04-12 Robert Bosch Gmbh Verfahren zur einstellung einer temperatur eines sensorelements

Family Cites Families (50)

* 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
JP2002529499A (ja) 1998-11-13 2002-09-10 イーライ・リリー・アンド・カンパニー 痛みの治療方法
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
WO2002100353A2 (en) 2001-06-11 2002-12-19 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
EP1531844B1 (en) 2002-02-22 2014-08-20 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
MXPA05009757A (es) 2003-03-13 2005-12-05 Controlled Chemicals Inc Conjugados de oxicodona con menor potencial de abuso y duracion de accion extendida.
EP1782834A3 (en) 2003-03-13 2007-08-01 Controlled Chemicals, Inc. Oxycodone conjugates with lower abuse potential and extended duration of action
EP1644019B2 (en) 2003-05-29 2018-02-21 Shire LLC Abuse resistant amphetamine compounds
EP1675555A4 (en) 2003-09-30 2011-03-09 Shire Llc PHARMACEUTICAL COMPOSITIONS FOR PREVENTING EXCESSIVE DOSE OR ABUSE
EP1928881A2 (en) * 2005-08-19 2008-06-11 Pharmacofore, Inc. Prodrugs of active agents
EP2056800B1 (en) 2005-08-26 2015-12-09 The Board Of Trustees Of The Leland Stanford Junior University Therapy procedure for drug delivery for trigeminal pain
CA2624179A1 (en) 2005-10-06 2007-04-12 Auspex Pharmaceuticals, Inc. Deuterated inhibitors of gastric h+, k+-atpase with enhanced therapeutic properties
PL1959948T3 (pl) 2005-12-05 2012-12-31 Xenoport Inc Metanosulfonian proleku lewodopy, jego kompozycje, oraz jego zastosowania
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
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
DK2046393T3 (da) 2006-05-26 2014-05-12 Signature Therapeutics Inc Kontrolleret frigivelse af phenol-opioider
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
WO2008101202A1 (en) 2007-02-16 2008-08-21 Pharmacofore, Inc. N-17-alkylated prodrugs of opioids
WO2008101187A2 (en) 2007-02-16 2008-08-21 Pharmacofore, Inc. Pro-drugs of peripheral phenolic opioid antagonists
CN104958282B (zh) 2007-11-23 2018-05-29 格吕伦塔尔有限公司 他喷他多组合物
US9023860B2 (en) 2007-11-26 2015-05-05 Signature Therapeutics, Inc. Pro-drugs for controlled release of biologically active compounds
CA2714331C (en) 2008-02-14 2016-08-09 Alkermes, Inc. Selective opioid compounds
AU2009305563C1 (en) * 2008-10-17 2015-09-03 Signature Therapeutics, 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
CN102573845A (zh) 2009-04-02 2012-07-11 夏尔有限责任公司 新的阿片样物质的二羧酸连接的氨基酸和肽前药及其用途
KR20120060203A (ko) * 2009-07-17 2012-06-11 엘엘씨 샤이어 신규한 오피오이드의 카바메이트 아미노산과 펩티드 프로드럭 및 그의 용도
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
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
WO2011133348A1 (en) 2010-04-21 2011-10-27 Pharmacofore, Inc. Compositions comprising enzyme-cleavable amphetamine prodrugs and inhibitors thereof
WO2011133178A1 (en) 2010-04-21 2011-10-27 Pharmacofore, Inc Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug
US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
WO2011133346A1 (en) 2010-04-21 2011-10-27 Pharmacofore, Inc. Peripheral opioid agonists and peripheral opioid antagonists
CN103384472B (zh) 2011-01-11 2016-01-20 特色疗法股份有限公司 包含酶可裂解的羟考酮药物前体的组合物
WO2012096886A1 (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
WO2012122420A2 (en) 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012045599A1 (de) * 2010-10-06 2012-04-12 Robert Bosch Gmbh Verfahren zur einstellung einer temperatur eines sensorelements

Also Published As

Publication number Publication date
CN103813800B (zh) 2017-12-19
US20140121152A1 (en) 2014-05-01
EP2683394A2 (en) 2014-01-15
IL228215B (en) 2019-01-31
JP2014518546A (ja) 2014-07-31
BR112013022946A2 (pt) 2017-07-18
RU2608305C2 (ru) 2017-01-17
US9139612B2 (en) 2015-09-22
JP6148182B2 (ja) 2017-06-14
CN103813800A (zh) 2014-05-21
WO2012122422A2 (en) 2012-09-13
CA2827662C (en) 2020-07-14
EP2683394A4 (en) 2015-06-03
US20160002291A1 (en) 2016-01-07
EP2683394B1 (en) 2021-01-06
WO2012122422A3 (en) 2014-04-24
RU2013144368A (ru) 2015-04-10
CA2827662A1 (en) 2012-09-13
AU2012225337A1 (en) 2013-05-09

Similar Documents

Publication Publication Date Title
AU2012225337B2 (en) Active agent prodrugs with heterocyclic linkers
US9095627B2 (en) Opioid prodrugs with heterocyclic linkers
US10028945B2 (en) Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
AU2010351605C1 (en) Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
WO2011133150A1 (en) Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof
HK1193976B (en) Active agent prodrugs with heterocyclic linkers
HK1193976A (en) Active agent prodrugs with heterocyclic linkers
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
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)