JP2013503862A - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP2013503862A JP2013503862A JP2012527871A JP2012527871A JP2013503862A JP 2013503862 A JP2013503862 A JP 2013503862A JP 2012527871 A JP2012527871 A JP 2012527871A JP 2012527871 A JP2012527871 A JP 2012527871A JP 2013503862 A JP2013503862 A JP 2013503862A
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- aryl
- hydrogen
- ketone
- 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.)
- Pending
Links
- DZOJGFYNVJBHRH-DFAGXDKMSA-N C[C@H](C1(CC=C(C2)OC(N(C)CCNC(C3(C(CCNC(N)=N)C3)NC(CC(O)=O)=O)=O)=O)O)N(C)CC[C@@]12c1c(C)ccc(OC)c1O Chemical compound C[C@H](C1(CC=C(C2)OC(N(C)CCNC(C3(C(CCNC(N)=N)C3)NC(CC(O)=O)=O)=O)=O)O)N(C)CC[C@@]12c1c(C)ccc(OC)c1O DZOJGFYNVJBHRH-DFAGXDKMSA-N 0.000 description 1
Classifications
-
- 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
-
- 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:
- C07D489/02—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 oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
-
- 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
- A61K31/495—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
-
- 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
- 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
- A61K47/54—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 an organic compound
-
- 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
- A61K47/54—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 an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P25/36—Opioid-abuse
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (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)
- Peptides Or Proteins (AREA)
- Medicines Containing Plant Substances (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24061109P | 2009-09-08 | 2009-09-08 | |
| US61/240,611 | 2009-09-08 | ||
| US28814809P | 2009-12-18 | 2009-12-18 | |
| US61/288,148 | 2009-12-18 | ||
| PCT/US2010/031956 WO2011031350A1 (en) | 2009-09-08 | 2010-04-21 | Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015190867A Division JP2016041698A (ja) | 2009-09-08 | 2015-09-29 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013503862A true JP2013503862A (ja) | 2013-02-04 |
| JP2013503862A5 JP2013503862A5 (https=) | 2013-06-06 |
Family
ID=43732738
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012527871A Pending JP2013503862A (ja) | 2009-09-08 | 2010-04-21 | 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 |
| JP2015190867A Pending JP2016041698A (ja) | 2009-09-08 | 2015-09-29 | 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 |
| JP2018100108A Active JP6778234B2 (ja) | 2009-09-08 | 2018-05-25 | 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 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015190867A Pending JP2016041698A (ja) | 2009-09-08 | 2015-09-29 | 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 |
| JP2018100108A Active JP6778234B2 (ja) | 2009-09-08 | 2018-05-25 | 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 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9493477B2 (https=) |
| EP (1) | EP2475429B1 (https=) |
| JP (3) | JP2013503862A (https=) |
| CN (1) | CN102695545B (https=) |
| AU (1) | AU2010293028B2 (https=) |
| BR (1) | BR112012005124B1 (https=) |
| CA (1) | CA2773340C (https=) |
| IL (1) | IL218498A (https=) |
| MX (1) | MX348262B (https=) |
| PH (1) | PH12012500485A1 (https=) |
| RU (1) | RU2600736C2 (https=) |
| SG (1) | SG179026A1 (https=) |
| WO (1) | WO2011031350A1 (https=) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014502972A (ja) * | 2011-01-11 | 2014-02-06 | シグネーチャー セラピューティクス，インク． | 酵素切断可能なオキシコドンプロドラッグを含んでなる組成物 |
| JP2021504351A (ja) * | 2017-11-24 | 2021-02-15 | ビョンディス・ビー．ブイ．Ｂｙｏｎｄｉｓ Ｂ．Ｖ． | リンカー薬物化合物ｖｃ−ｓｅｃｏ−ＤＵＢＡ製造のための改善された方法 |
| JP2021532183A (ja) * | 2018-07-27 | 2021-11-25 | コンセントリック アナルジェジクス，インク． | フェノール性ｔｒｐｖ１アゴニストのｐｅｇ化プロドラッグ |
| 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 |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102695545B (zh) * | 2009-09-08 | 2016-08-17 | 特色疗法股份有限公司 | 包括酶可剪切的酮改性的阿片样物质药物前体以及其可任选的抑制剂的组合物 |
| CA2795222A1 (en) * | 2010-04-21 | 2011-10-27 | Signature Therapeutics, Inc. | 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 |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US9700508B2 (en) | 2010-05-10 | 2017-07-11 | Euro-Celtique S.A. | Pharmaceutical compositions comprising hydromorphone and naloxone |
| PH12012502083A1 (en) | 2010-05-10 | 2017-07-26 | Euro Celtique Sa | Manufacturing of active-free granules and tablets comprising the same |
| EP2568965A1 (en) | 2010-05-10 | 2013-03-20 | Euro-Celtique S.A. | Combination of active loaded granules with additional actives |
| WO2012122420A2 (en) | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
| JP6148182B2 (ja) | 2011-03-09 | 2017-06-14 | シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. | 複素環式リンカーを有する活性薬剤プロドラッグ |
| US9605296B2 (en) * | 2011-09-29 | 2017-03-28 | Ecole Normale Superieure De Lyon | Fluorogenic peptidase substrate |
| SG11201401856VA (en) | 2011-10-26 | 2014-05-29 | Kempharm Inc | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof |
| WO2015071380A1 (en) | 2013-11-13 | 2015-05-21 | Euro-Celtique S.A. | Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome |
| US10626156B2 (en) | 2013-12-06 | 2020-04-21 | Jie Han | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| RU2683274C2 (ru) | 2014-12-02 | 2019-03-27 | Кемфарм, Инк. | Бензойная кислота, производные бензойной кислоты и конъюгаты гетероарилкарбоновой кислоты и оксиморфона, их пролекарства, способы получения и применение |
| WO2020012245A1 (en) | 2018-07-13 | 2020-01-16 | Alkermes Pharma Ireland Limited | Thienothiophene-naltrexone prodrugs for long-acting injectable compositions |
| US10799496B2 (en) | 2018-07-13 | 2020-10-13 | Alkermes Pharma Ireland Limited | Naphthylenyl compounds for long-acting injectable compositions and related methods |
| US10975099B2 (en) | 2018-11-05 | 2021-04-13 | Alkermes Pharma Ireland Limited | Thiophene compounds for long-acting injectable compositions and related methods |
| CN113624665A (zh) * | 2021-07-30 | 2021-11-09 | 中国药科大学 | 一种抗肿瘤候选化合物在治疗结直肠癌药物中的应用及测定方法 |
| CA3230025A1 (en) | 2021-09-29 | 2023-04-06 | Lynn Kirkpatrick | Enzyme-cleavable methadone prodrugs and methods of use thereof |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050176644A1 (en) * | 2003-09-30 | 2005-08-11 | New River Pharmaceuticals Inc. | Compounds and compositions for prevention of overdose of oxycodone |
| JP2007507520A (ja) * | 2003-09-30 | 2007-03-29 | ニュー リバー ファーマシューティカルズ インコーポレイテッド | 過剰摂取又は乱用を防止するための薬学組成物 |
| WO2007120648A2 (en) * | 2006-04-10 | 2007-10-25 | 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 |
| WO2007140272A2 (en) * | 2006-05-26 | 2007-12-06 | Pharmacofore, Inc. | Controlled release of phenolic opioids |
| US20090137618A1 (en) * | 2007-11-26 | 2009-05-28 | Jenkins Thomas E | Pro-drugs for controlled release of biologically active compounds |
| JP2012509846A (ja) * | 2008-10-17 | 2012-04-26 | ファーマコフォア，インク． | フェノール性オピオイドの放出が減弱された医薬組成物 |
| JP2013525348A (ja) * | 2010-04-21 | 2013-06-20 | 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 |
Family Cites Families (37)
| 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 |
| 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 |
| US6388122B1 (en) | 1996-04-10 | 2002-05-14 | Ono Pharmaceutical Co., Ltd. | Tryptase inhibitor and novel guanidino derivatives |
| ATE441725T1 (de) | 1998-12-15 | 2009-09-15 | Applera Corp | Multienzym-nachweisverfahren |
| DE60011053T2 (de) | 1999-02-18 | 2005-05-25 | SuperGen, Inc., Dublin | 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 |
| 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 |
| US7375082B2 (en) * | 2002-02-22 | 2008-05-20 | Shire Llc | Abuse-resistant hydrocodone compounds |
| RU2215741C1 (ru) * | 2002-11-05 | 2003-11-10 | Открытое Акционерное Общество "Международная Научно-Технологическая Корпорация" | Сложные эфиры n-замещенных 14-гидроксиморфинанов и способ их получения |
| US20100092562A1 (en) | 2002-11-26 | 2010-04-15 | Hollenbeck R Gary | Sustained-release drug delivery compositions and methods |
| SI1644019T2 (en) | 2003-05-29 | 2018-04-30 | Shire Llc | Abuse resistant amphetamine compounds |
| WO2005042773A1 (en) | 2003-10-24 | 2005-05-12 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
| FR2881363B1 (fr) * | 2005-02-02 | 2008-03-14 | Commissariat Energie Atomique | Dispositif d'analyses biologiques avec detecteur integre |
| US8163701B2 (en) | 2005-08-19 | 2012-04-24 | Signature Therapeutics, Inc. | Prodrugs of active agents |
| JP5276982B2 (ja) | 2005-08-26 | 2013-08-28 | ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ | オキシトシンの投与による頭痛の処置のための方法 |
| EP1934201A1 (en) | 2005-10-06 | 2008-06-25 | Auspex Pharmaceuticals Inc. | Deuterated inhibitors of gastric h+, k+-atpase with enhanced therapeutic properties |
| US7563821B2 (en) | 2005-12-05 | 2009-07-21 | Xenoport, Inc. | Levodopa prodrug mesylate, compositions thereof, and uses thereof |
| US20110105381A2 (en) | 2007-02-16 | 2011-05-05 | Pharmacofore, Inc. | Prodrugs of Peripheral Phenolic Opioid Antagonists |
| WO2008101202A1 (en) | 2007-02-16 | 2008-08-21 | Pharmacofore, Inc. | N-17-alkylated prodrugs of opioids |
| 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 |
| ES2671897T3 (es) | 2008-02-14 | 2018-06-11 | Alkermes, Inc. | Compuestos opioides selectivos |
| US20110046053A1 (en) | 2008-05-05 | 2011-02-24 | Oramed Ltd. | Methods and compositions for oral administration of exenatide |
| BRPI1015108A2 (pt) | 2009-04-02 | 2016-04-26 | Shire Llc | pró-fármacos de aminoácidos e peptídios ligados a ácido dicarboxílico de opiáceos e seus usos |
| WO2011007247A1 (en) | 2009-07-17 | 2011-01-20 | Llc Shire | Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof |
| CN102695545B (zh) * | 2009-09-08 | 2016-08-17 | 特色疗法股份有限公司 | 包括酶可剪切的酮改性的阿片样物质药物前体以及其可任选的抑制剂的组合物 |
| 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 |
| US8497237B2 (en) | 2011-01-11 | 2013-07-30 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| AU2012205733B2 (en) | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| JP6148182B2 (ja) * | 2011-03-09 | 2017-06-14 | シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. | 複素環式リンカーを有する活性薬剤プロドラッグ |
| WO2012122420A2 (en) * | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
-
2010
- 2010-04-21 CN CN201080048158.6A patent/CN102695545B/zh active Active
- 2010-04-21 JP JP2012527871A patent/JP2013503862A/ja active Pending
- 2010-04-21 AU AU2010293028A patent/AU2010293028B2/en active Active
- 2010-04-21 US US13/393,470 patent/US9493477B2/en active Active
- 2010-04-21 BR BR112012005124-5A patent/BR112012005124B1/pt active IP Right Grant
- 2010-04-21 WO PCT/US2010/031956 patent/WO2011031350A1/en not_active Ceased
- 2010-04-21 EP EP10815769.4A patent/EP2475429B1/en active Active
- 2010-04-21 PH PH1/2012/500485A patent/PH12012500485A1/en unknown
- 2010-04-21 MX MX2012002847A patent/MX348262B/es active IP Right Grant
- 2010-04-21 SG SG2012016036A patent/SG179026A1/en unknown
- 2010-04-21 RU RU2012108874/04A patent/RU2600736C2/ru active
- 2010-04-21 CA CA2773340A patent/CA2773340C/en active Active
-
2012
- 2012-03-06 IL IL218498A patent/IL218498A/en active IP Right Grant
-
2015
- 2015-09-29 JP JP2015190867A patent/JP2016041698A/ja active Pending
-
2016
- 2016-10-05 US US15/285,818 patent/US10028945B2/en active Active
-
2018
- 2018-05-25 JP JP2018100108A patent/JP6778234B2/ja active Active
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050176644A1 (en) * | 2003-09-30 | 2005-08-11 | New River Pharmaceuticals Inc. | Compounds and compositions for prevention of overdose of oxycodone |
| JP2007507520A (ja) * | 2003-09-30 | 2007-03-29 | ニュー リバー ファーマシューティカルズ インコーポレイテッド | 過剰摂取又は乱用を防止するための薬学組成物 |
| WO2007120648A2 (en) * | 2006-04-10 | 2007-10-25 | 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 |
| WO2007140272A2 (en) * | 2006-05-26 | 2007-12-06 | Pharmacofore, Inc. | Controlled release of phenolic opioids |
| US20090137618A1 (en) * | 2007-11-26 | 2009-05-28 | Jenkins Thomas E | Pro-drugs for controlled release of biologically active compounds |
| JP2012509846A (ja) * | 2008-10-17 | 2012-04-26 | ファーマコフォア，インク． | フェノール性オピオイドの放出が減弱された医薬組成物 |
| JP2013525348A (ja) * | 2010-04-21 | 2013-06-20 | 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 |
Non-Patent Citations (1)
| Title |
|---|
| JPN6014017363; Ｂｉｏｏｒｇａｎｉｃ Ｃｈｅｍｉｓｔｒｙ ３０, 2002, ｐ．２８５-３０１ * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014502972A (ja) * | 2011-01-11 | 2014-02-06 | シグネーチャー セラピューティクス，インク． | 酵素切断可能なオキシコドンプロドラッグを含んでなる組成物 |
| JP2021504351A (ja) * | 2017-11-24 | 2021-02-15 | ビョンディス・ビー．ブイ．Ｂｙｏｎｄｉｓ Ｂ．Ｖ． | リンカー薬物化合物ｖｃ−ｓｅｃｏ−ＤＵＢＡ製造のための改善された方法 |
| JP7279042B2 (ja) | 2017-11-24 | 2023-05-22 | ビョンディス・ビー．ブイ． | リンカー薬物化合物ｖｃ－ｓｅｃｏ－ＤＵＢＡ製造のための改善された方法 |
| JP2021532183A (ja) * | 2018-07-27 | 2021-11-25 | コンセントリック アナルジェジクス，インク． | フェノール性ｔｒｐｖ１アゴニストのｐｅｇ化プロドラッグ |
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010293028B2 (en) | 2014-12-18 |
| US20120230916A1 (en) | 2012-09-13 |
| MX2012002847A (es) | 2012-08-23 |
| BR112012005124A2 (pt) | 2020-08-25 |
| AU2010293028A1 (en) | 2012-04-05 |
| WO2011031350A1 (en) | 2011-03-17 |
| BR112012005124B1 (pt) | 2021-11-09 |
| EP2475429A4 (en) | 2013-04-03 |
| SG179026A1 (en) | 2012-04-27 |
| JP2018172387A (ja) | 2018-11-08 |
| JP6778234B2 (ja) | 2020-10-28 |
| US9493477B2 (en) | 2016-11-15 |
| HK1172283A1 (zh) | 2013-04-19 |
| CN102695545A (zh) | 2012-09-26 |
| RU2012108874A (ru) | 2013-09-20 |
| CA2773340A1 (en) | 2011-03-17 |
| PH12012500485A1 (en) | 2012-10-22 |
| EP2475429B1 (en) | 2015-07-29 |
| RU2600736C2 (ru) | 2016-10-27 |
| US20170119754A1 (en) | 2017-05-04 |
| CA2773340C (en) | 2019-07-23 |
| IL218498A (en) | 2017-03-30 |
| CN102695545B (zh) | 2016-08-17 |
| JP2016041698A (ja) | 2016-03-31 |
| US10028945B2 (en) | 2018-07-24 |
| EP2475429A1 (en) | 2012-07-18 |
| MX348262B (es) | 2017-06-05 |
| IL218498A0 (en) | 2012-07-31 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| 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 | |
| JP6148182B2 (ja) | 複素環式リンカーを有する活性薬剤プロドラッグ | |
| US9095627B2 (en) | Opioid prodrugs with heterocyclic linkers | |
| 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 | |
| US9238020B2 (en) | Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug | |
| US20110262360A1 (en) | Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof | |
| 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 | |
| HK1193976B (en) | Active agent prodrugs with heterocyclic linkers | |
| HK1193976A (en) | Active agent prodrugs with heterocyclic linkers |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20130417 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20130417 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20140529 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20140606 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20140821 |
|
| A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20140828 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20141208 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20150529 |