CO2017005201A2 - Ácido benzóico, derivados de ácido benzóico y conjugados heteroarilcarboxílico de la oxicodona - Google Patents
Ácido benzóico, derivados de ácido benzóico y conjugados heteroarilcarboxílico de la oxicodonaInfo
- Publication number
- CO2017005201A2 CO2017005201A2 CONC2017/0005201A CO2017005201A CO2017005201A2 CO 2017005201 A2 CO2017005201 A2 CO 2017005201A2 CO 2017005201 A CO2017005201 A CO 2017005201A CO 2017005201 A2 CO2017005201 A2 CO 2017005201A2
- Authority
- CO
- Colombia
- Prior art keywords
- oxycodone
- benzoic acid
- conjugates
- heteroarylcarboxylic
- acid derivatives
- Prior art date
Links
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 title abstract 4
- 229960002085 oxycodone Drugs 0.000 title abstract 4
- 150000001558 benzoic acid derivatives Chemical class 0.000 title abstract 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 title 2
- 239000005711 Benzoic acid Substances 0.000 title 1
- 235000010233 benzoic acid Nutrition 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical class CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 abstract 1
- 150000001242 acetic acid derivatives Chemical class 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 229940111136 antiinflammatory and antirheumatic drug fenamates Drugs 0.000 abstract 1
- -1 fenamates Chemical class 0.000 abstract 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 abstract 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003873 salicylate salts Chemical class 0.000 abstract 1
- 230000002194 synthesizing effect Effects 0.000 abstract 1
Classifications
-
- 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
- C07D489/04—Salts; Organic complexes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Addiction (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La a tecnología actualmente descrita proporciona composiciones que comprenden ácidos arilcarboxílicos y, por ejemplo, AINES, químicamente conjugados a la oxicodona (4,5-α-epoxi-14-hidroxi-17-metilmorfinan-6-ona) para formar nuevos profármacos/composiciones de la oxicodona, incluyendo benzoatos, salicilatos, propionatos, fenamatos y acetatos, que tienen un menor potencial de abuso de la oxicodona. La presente tecnología también proporciona métodos para el tratamiento de pacientes, kits farmacéuticos y métodos para sintetizar conjugados de la presente tecnología.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462084216P | 2014-11-25 | 2014-11-25 | |
US201462084246P | 2014-11-25 | 2014-11-25 | |
PCT/US2015/062637 WO2016086113A1 (en) | 2014-11-25 | 2015-11-25 | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone |
Publications (1)
Publication Number | Publication Date |
---|---|
CO2017005201A2 true CO2017005201A2 (es) | 2017-08-31 |
Family
ID=56075034
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CONC2017/0005201A CO2017005201A2 (es) | 2014-11-25 | 2017-05-25 | Ácido benzóico, derivados de ácido benzóico y conjugados heteroarilcarboxílico de la oxicodona |
Country Status (18)
Country | Link |
---|---|
US (3) | US9850252B2 (es) |
EP (1) | EP3223819A4 (es) |
JP (2) | JP6400848B2 (es) |
KR (2) | KR101976101B1 (es) |
CN (1) | CN106999486A (es) |
AU (1) | AU2015353502B2 (es) |
BR (1) | BR112017011069A2 (es) |
CA (1) | CA2967424C (es) |
CL (1) | CL2017001353A1 (es) |
CO (1) | CO2017005201A2 (es) |
IL (1) | IL252470B (es) |
MX (1) | MX2017006520A (es) |
NZ (1) | NZ731591A (es) |
PH (1) | PH12017500963A1 (es) |
RU (1) | RU2683317C2 (es) |
SG (1) | SG11201704178UA (es) |
WO (1) | WO2016086113A1 (es) |
ZA (1) | ZA201703154B (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
US10849981B2 (en) | 2009-07-02 | 2020-12-01 | KemPham, Inc. | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof |
NZ731591A (en) | 2014-11-25 | 2018-06-29 | Kempharm Inc | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone |
US20200038383A1 (en) * | 2016-10-14 | 2020-02-06 | Kempharm, Inc. | Immediate-release abuse deterrent compositions or medicaments for treating pain, add, adhd and other syndromes or disorders |
US11254685B2 (en) | 2017-07-20 | 2022-02-22 | Suzhou Runxindatai Pharmaceutics Ltd Co. | Abuse-resistant long-acting release opioid prodrugs |
EP3755704A1 (en) * | 2018-02-23 | 2020-12-30 | Rhodes Technologies Inc. | Novel opioid compounds and uses thereof |
Family Cites Families (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB320749A (es) | ||||
US1731152A (en) | 1925-10-27 | 1929-10-08 | Firm C H Boehringer Sohn | Process for the manufacture of derivatives of dihydrocodeinone or its substitution products |
AT229496B (de) | 1961-03-08 | 1963-09-25 | Lannacher Heilmittel | Verfahren zur Darstellung des neuen Nicotinsäureesters des Dihydrohydroxycodeinons |
US4668685A (en) | 1984-07-05 | 1987-05-26 | E.I. Du Pont De Nemours And Company | Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists |
SE9003665D0 (sv) | 1990-11-16 | 1990-11-16 | Kabivitrum Ab | Morphine prodrugs |
GB9423542D0 (en) | 1994-11-22 | 1995-01-11 | Marples Brian A | Pharmaceutical compounds |
US5869669A (en) * | 1996-07-26 | 1999-02-09 | Penick Corporation | Preparation of 14-hydroxynormorphinones from normorphinone dienol acylates |
JP2004501067A (ja) | 2000-01-28 | 2004-01-15 | ローム アンド ハース カンパニー | 高められた特性をもつ医薬 |
KR20040014544A (ko) | 2001-06-05 | 2004-02-14 | 컨트롤 딜리버리 시스템즈 인코포레이티드 | 서방 진통제 화합물 |
US7375083B2 (en) | 2003-09-30 | 2008-05-20 | Shire Llc | Pharmaceutical compositions for prevention of overdose or abuse |
US7375082B2 (en) | 2002-02-22 | 2008-05-20 | Shire Llc | Abuse-resistant hydrocodone compounds |
IL163667A0 (en) | 2002-02-22 | 2005-12-18 | New River Pharmaceuticals Inc | Novel sustained release pharmaceutical compounds to preventabuse of controlled substances |
US20040058946A1 (en) * | 2002-07-05 | 2004-03-25 | Buchwald Stephen L. | Abuse-resistant prodrugs of oxycodone and other pharmaceuticals |
TW200500067A (en) | 2003-01-21 | 2005-01-01 | Control Delivery Sys Inc | Salts of codrugs and uses related thereto |
ATE454169T1 (de) * | 2003-03-13 | 2010-01-15 | Controlled Chemicals Inc | Oxycodon- konjugate mit niedrigerem missbrauch- potential und ausgedehnter tätigkeitsdauer |
EP1782834A3 (en) * | 2003-03-13 | 2007-08-01 | Controlled Chemicals, Inc. | Oxycodone conjugates with lower abuse potential and extended duration of action |
WO2005034859A2 (en) * | 2003-10-03 | 2005-04-21 | Elite Laboratories Inc. | Extended release formulations of opioids and method of use thereof |
US20050203115A1 (en) * | 2004-03-10 | 2005-09-15 | Sancilio Frederick D. | Narcotic-NSAID ion pairs |
PT1751087E (pt) | 2004-06-04 | 2012-09-10 | Xenoport Inc | Derivados de levodopa e as suas composições e utilizações |
US7348430B2 (en) | 2005-01-21 | 2008-03-25 | Acura Pharmaceuticals, Inc. | Production of opioid analgesics |
WO2007120648A2 (en) * | 2006-04-10 | 2007-10-25 | Shire Llc | Mono and di-substituted oxycodone compounds and compositions |
RU2469038C2 (ru) | 2006-05-26 | 2012-12-10 | Фармакофор, Инк. | Контролируемое высвобождение фенольных опиатов |
US20080090771A1 (en) | 2006-10-06 | 2008-04-17 | Shire Llc | Abuse-resistant hydrocodone compounds, compositions and methods of using the same |
US8067596B2 (en) | 2007-12-17 | 2011-11-29 | Mallinckrodt Llc | Processes for the production of (+)- “Nal” morphinan compounds |
AU2010266209B2 (en) | 2009-07-02 | 2013-09-26 | Kempharm, Inc. | Phenylethanoic acid, phenylpropanoic acid and phenylpropenoic acid conjugates and prodrugs of hydrocodone, methods of making and use thereof |
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 |
US8623888B2 (en) | 2009-07-15 | 2014-01-07 | Mallinckrodt Llc | 3-oxy-hydromorphone derivatives |
AU2012205733B2 (en) * | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
RU2573388C2 (ru) * | 2011-10-26 | 2016-01-20 | Кемфарм Инк. | Бензойная кислота, производные бензойной кислоты и конъюгаты гетероарилкарбоновой кислоты с гидроморфоном, пролекарства, способы получения и их применение |
NZ731591A (en) | 2014-11-25 | 2018-06-29 | Kempharm Inc | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone |
-
2015
- 2015-11-25 NZ NZ731591A patent/NZ731591A/en not_active IP Right Cessation
- 2015-11-25 WO PCT/US2015/062637 patent/WO2016086113A1/en active Application Filing
- 2015-11-25 RU RU2017122144A patent/RU2683317C2/ru not_active IP Right Cessation
- 2015-11-25 BR BR112017011069A patent/BR112017011069A2/pt not_active Application Discontinuation
- 2015-11-25 AU AU2015353502A patent/AU2015353502B2/en not_active Ceased
- 2015-11-25 CA CA2967424A patent/CA2967424C/en active Active
- 2015-11-25 CN CN201580064309.XA patent/CN106999486A/zh active Pending
- 2015-11-25 JP JP2017528967A patent/JP6400848B2/ja not_active Expired - Fee Related
- 2015-11-25 EP EP15863639.9A patent/EP3223819A4/en not_active Withdrawn
- 2015-11-25 KR KR1020177017408A patent/KR101976101B1/ko active IP Right Grant
- 2015-11-25 SG SG11201704178UA patent/SG11201704178UA/en unknown
- 2015-11-25 KR KR1020197012631A patent/KR20190049944A/ko active Application Filing
- 2015-11-25 US US14/952,348 patent/US9850252B2/en active Active
- 2015-11-25 MX MX2017006520A patent/MX2017006520A/es unknown
-
2017
- 2017-05-08 ZA ZA2017/03154A patent/ZA201703154B/en unknown
- 2017-05-23 IL IL252470A patent/IL252470B/en not_active IP Right Cessation
- 2017-05-25 PH PH12017500963A patent/PH12017500963A1/en unknown
- 2017-05-25 CL CL2017001353A patent/CL2017001353A1/es unknown
- 2017-05-25 CO CONC2017/0005201A patent/CO2017005201A2/es unknown
- 2017-11-14 US US15/812,730 patent/US10144740B2/en active Active
-
2018
- 2018-09-04 JP JP2018165325A patent/JP2018199719A/ja active Pending
- 2018-10-19 US US16/165,194 patent/US10544153B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
US10144740B2 (en) | 2018-12-04 |
EP3223819A4 (en) | 2018-04-25 |
CA2967424A1 (en) | 2016-06-02 |
IL252470B (en) | 2019-08-29 |
JP2017535593A (ja) | 2017-11-30 |
US9850252B2 (en) | 2017-12-26 |
KR101976101B1 (ko) | 2019-05-09 |
JP2018199719A (ja) | 2018-12-20 |
WO2016086113A1 (en) | 2016-06-02 |
CL2017001353A1 (es) | 2018-01-05 |
JP6400848B2 (ja) | 2018-10-03 |
IL252470A0 (en) | 2017-07-31 |
CN106999486A (zh) | 2017-08-01 |
PH12017500963A1 (en) | 2017-10-18 |
AU2015353502B2 (en) | 2018-09-27 |
CA2967424C (en) | 2023-05-02 |
KR20170094249A (ko) | 2017-08-17 |
RU2017122144A (ru) | 2018-12-26 |
BR112017011069A2 (pt) | 2018-07-10 |
ZA201703154B (en) | 2019-03-27 |
RU2017122144A3 (es) | 2018-12-26 |
RU2683317C2 (ru) | 2019-03-28 |
EP3223819A1 (en) | 2017-10-04 |
AU2015353502A1 (en) | 2017-05-25 |
MX2017006520A (es) | 2017-08-09 |
KR20190049944A (ko) | 2019-05-09 |
NZ731591A (en) | 2018-06-29 |
SG11201704178UA (en) | 2017-06-29 |
US20190048018A1 (en) | 2019-02-14 |
US20160168160A1 (en) | 2016-06-16 |
US20180065975A1 (en) | 2018-03-08 |
US10544153B2 (en) | 2020-01-28 |
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