JP2013500256A5 - - Google Patents
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- Publication number
- JP2013500256A5 JP2013500256A5 JP2012521761A JP2012521761A JP2013500256A5 JP 2013500256 A5 JP2013500256 A5 JP 2013500256A5 JP 2012521761 A JP2012521761 A JP 2012521761A JP 2012521761 A JP2012521761 A JP 2012521761A JP 2013500256 A5 JP2013500256 A5 JP 2013500256A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- poly
- group
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 54
- 150000003839 salts Chemical class 0.000 claims description 34
- -1 methoxyphenyl Chemical group 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 16
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims description 8
- 239000005977 Ethylene Substances 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000002541 furyl group Chemical group 0.000 claims description 6
- 125000005059 halophenyl group Chemical group 0.000 claims description 6
- 150000002431 hydrogen Chemical class 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 6
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims description 6
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 125000001544 thienyl group Chemical group 0.000 claims description 6
- 125000005647 linker group Chemical group 0.000 claims description 5
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 8
- 239000000178 monomer Substances 0.000 claims 4
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000001412 amines Chemical class 0.000 description 8
- 125000004429 atom Chemical group 0.000 description 3
- 239000003402 opiate agonist Substances 0.000 description 3
- 229940127450 Opioid Agonists Drugs 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22739909P | 2009-07-21 | 2009-07-21 | |
| US61/227,399 | 2009-07-21 | ||
| US12/558,395 US8173666B2 (en) | 2007-03-12 | 2009-09-11 | Oligomer-opioid agonist conjugates |
| US12/558,395 | 2009-09-11 | ||
| US35085310P | 2010-06-02 | 2010-06-02 | |
| US61/350,853 | 2010-06-02 | ||
| PCT/US2010/042792 WO2011011543A1 (en) | 2009-07-21 | 2010-07-21 | Oligomer-opioid agonist conjugates |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015139389A Division JP2015180698A (ja) | 2009-07-21 | 2015-07-13 | オリゴマー−オピオイドアゴニスト抱合体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013500256A JP2013500256A (ja) | 2013-01-07 |
| JP2013500256A5 true JP2013500256A5 (enExample) | 2013-09-05 |
| JP5837491B2 JP5837491B2 (ja) | 2015-12-24 |
Family
ID=43499405
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012521761A Expired - Fee Related JP5837491B2 (ja) | 2009-07-21 | 2010-07-21 | オリゴマー−オピオイドアゴニスト抱合体 |
| JP2015139389A Pending JP2015180698A (ja) | 2009-07-21 | 2015-07-13 | オリゴマー−オピオイドアゴニスト抱合体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015139389A Pending JP2015180698A (ja) | 2009-07-21 | 2015-07-13 | オリゴマー−オピオイドアゴニスト抱合体 |
Country Status (9)
| Country | Link |
|---|---|
| EP (2) | EP2628489B1 (enExample) |
| JP (2) | JP5837491B2 (enExample) |
| KR (1) | KR101788886B1 (enExample) |
| CN (1) | CN102573918A (enExample) |
| AU (1) | AU2010276244B2 (enExample) |
| CA (1) | CA2768392C (enExample) |
| IL (3) | IL217634B (enExample) |
| MX (1) | MX2012000980A (enExample) |
| WO (1) | WO2011011543A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10512644B2 (en) | 2007-03-12 | 2019-12-24 | Inheris Pharmaceuticals, Inc. | Oligomer-opioid agonist conjugates |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| EA023929B1 (ru) | 2010-09-30 | 2016-07-29 | Астразенека Аб | Кристаллический конъюгат налоксол-peg |
| CN103906522B (zh) * | 2011-11-07 | 2017-04-12 | 尼克塔治疗公司 | 阿片激动剂化合物和止痛化合物的组合物、剂型以及共给药 |
| US10525054B2 (en) | 2011-11-07 | 2020-01-07 | Inheris Biopharma, Inc. | Compositions, dosage forms, and co-administration of an opioid agonist compound and an analgesic compound |
| WO2014070745A1 (en) * | 2012-10-30 | 2014-05-08 | Nektar Therapeutics | Solid salt form of alpha-6-mpeg6-o-hydroxycodone as opioid agonists and uses thereof |
| ITRM20130223A1 (it) * | 2013-04-15 | 2014-10-16 | Rosario Nicoletti | Derivati della codeina come inibitori della glucuronazione della morfina |
| AU2014306759B2 (en) | 2013-08-12 | 2018-04-26 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| ES2809458T3 (es) | 2014-07-17 | 2021-03-04 | Pharmaceutical Manufacturing Res Services Inc | Forma de dosificación llena de líquido, disuasoria del abuso y de liberación inmediata |
| WO2016064873A1 (en) | 2014-10-20 | 2016-04-28 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| CN107019803B (zh) * | 2016-01-29 | 2020-09-15 | 北京键凯科技股份有限公司 | 具有低成瘾作用的聚乙二醇化阿片样物质 |
| CN107033154B (zh) | 2016-02-02 | 2020-02-04 | 上海瀚迈生物医药科技有限公司 | 阿片受体拮抗剂缀合物及其应用 |
| US11680137B2 (en) | 2018-03-29 | 2023-06-20 | Nof Corporation | Method for purifying trityl group-containing monodispersed polyethylene glycol |
| CN111039764A (zh) * | 2018-10-12 | 2020-04-21 | 山东大学 | 一种双亲乙烯衍生物及制备方法 |
| WO2021029914A1 (en) * | 2019-08-11 | 2021-02-18 | Kappa-Pharma LLC | Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates |
| CN116925105B (zh) * | 2022-04-11 | 2025-11-25 | 上海瀚迈生物医药科技有限公司 | 阿片受体拮抗剂缀合物的固体盐型、晶型及其制备方法、组合物和用途 |
| CN117567477A (zh) * | 2023-11-15 | 2024-02-20 | 宜昌人福药业有限责任公司 | 一种氢吗啡酮和二氢吗啡类药物低分子聚乙二醇化物及其制备方法和应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2654756A (en) | 1949-10-20 | 1953-10-06 | Mallinckrodt Chemical Works | Process of preparing codeinone, dihydrocodeinone, and dihydromorphinone |
| US2628962A (en) | 1949-10-20 | 1953-02-17 | Mallinckrodt Chemical Works | Method for preparing dihydrocodeinone, dihydromorphinone, and codeinone |
| US2649454A (en) | 1951-08-20 | 1953-08-18 | Univ California | Method for preparing dihydromorphinone, dihydrocodeinone, and dihydropseudocodeinone |
| US2806033A (en) | 1955-08-03 | 1957-09-10 | Lewenstein | Morphine derivative |
| AU6044496A (en) * | 1995-06-05 | 1996-12-24 | Cortech, Inc. | Compounds having bradykinin antagonistic activity and mu-opi oid agonistic activity |
| US5672662A (en) | 1995-07-07 | 1997-09-30 | Shearwater Polymers, Inc. | Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications |
| US6835802B2 (en) | 2001-06-04 | 2004-12-28 | Nobex Corporation | Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties |
| EP1782834A3 (en) * | 2003-03-13 | 2007-08-01 | Controlled Chemicals, Inc. | Oxycodone conjugates with lower abuse potential and extended duration of action |
| EP2905033B1 (en) | 2003-12-16 | 2020-09-02 | Nektar Therapeutics | Monodisperse PEGylated naloxol compositions |
| RS53937B1 (sr) * | 2007-03-12 | 2015-08-31 | Nektar Therapeutics | Konjugati oligomerno-opioidnog agonista |
| JP5827123B2 (ja) * | 2008-09-16 | 2015-12-02 | ウェルズ ファーゴ バンク ナショナル アソシエイション | 乱用の可能性が低いｐｅｇ化オピオイド |
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2010
- 2010-07-21 AU AU2010276244A patent/AU2010276244B2/en not_active Ceased
- 2010-07-21 JP JP2012521761A patent/JP5837491B2/ja not_active Expired - Fee Related
- 2010-07-21 EP EP13167519.1A patent/EP2628489B1/en active Active
- 2010-07-21 CA CA2768392A patent/CA2768392C/en not_active Expired - Fee Related
- 2010-07-21 KR KR1020127004344A patent/KR101788886B1/ko not_active Expired - Fee Related
- 2010-07-21 MX MX2012000980A patent/MX2012000980A/es active IP Right Grant
- 2010-07-21 EP EP10735413A patent/EP2456469A1/en not_active Withdrawn
- 2010-07-21 WO PCT/US2010/042792 patent/WO2011011543A1/en not_active Ceased
- 2010-07-21 CN CN2010800376109A patent/CN102573918A/zh active Pending
-
2012
- 2012-01-19 IL IL217634A patent/IL217634B/en active IP Right Grant
-
2015
- 2015-07-13 JP JP2015139389A patent/JP2015180698A/ja active Pending
-
2018
- 2018-01-09 IL IL256822A patent/IL256822B/en active IP Right Grant
- 2018-12-14 IL IL263713A patent/IL263713A/en unknown