ES2534055T3 - Opioides de amina no fenólicos con sustituyentes de gran tamaño - Google Patents
Opioides de amina no fenólicos con sustituyentes de gran tamaño Download PDFInfo
- Publication number
- ES2534055T3 ES2534055T3 ES09790652.3T ES09790652T ES2534055T3 ES 2534055 T3 ES2534055 T3 ES 2534055T3 ES 09790652 T ES09790652 T ES 09790652T ES 2534055 T3 ES2534055 T3 ES 2534055T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- aryl
- hydrogen
- optionally substituted
- alkoxy
- 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
Links
- 229940005483 opioid analgesics Drugs 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 14
- 125000003118 aryl group Chemical group 0.000 abstract 11
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 7
- -1 cyano, carbonyl Chemical group 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000304 alkynyl group Chemical group 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 abstract 2
- 239000004215 Carbon black (E152) Substances 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229930195733 hydrocarbon Natural products 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 abstract 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000005518 carboxamido group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000000470 constituent Substances 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 150000002430 hydrocarbons Chemical class 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 abstract 1
- 125000005592 polycycloalkyl group Polymers 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 1
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 abstract 1
- 150000003457 sulfones Chemical class 0.000 abstract 1
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 abstract 1
- 150000003462 sulfoxides Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/22—Bridged ring systems
- C07D221/26—Benzomorphans
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/34—Tobacco-abuse
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Abstract
Compuesto de fórmula I:**Fórmula** donde: R1 y R2 se seleccionan independientemente en cada caso entre hidrógeno y alquilo inferior opcionalmente sustituido; R3 se selecciona entre hidrógeno, hidrocarburo(C1-C8), heterociclilo, arilo e hidroxialquilo; R4 se selecciona entre hidrógeno, hidroxilo, alquilo(C1-C20) y alquilo(C1-C20) sustituido con hidroxilo o carbonilo; R5 es alquilo inferior; R6 es alquilo inferior; R7 se selecciona entre hidrógeno NR10R11 y -OR10; o R4, R5, R6 y R7 pueden formar juntos de uno a tres anillos, teniendo dichos anillos una sustitución adicional opcional; R8 y R8a son ambos iguales a hidrógeno o R8 y R8a juntos son >=O; R9 se selecciona entre hidrógeno y alquilo inferior; R10 y R11 son en cada caso, independientemente, hidrógeno, alquilo inferior opcionalmente sustituido, alquenilo opcionalmente sustituido, alquinilo opcionalmente sustituido, arilo opcionalmente sustituido, hidroxilo, amino o alcoxi inferior opcionalmente sustituido; y es -(C(R10)(R11))p- o un enlace directo, siendo p igual a 0, 1, 2, 3, 4, 5, 6 o 7; Y2 es un enlace directo o -(C(R10)(R11))q-, siendo q igual a 0, 1, 2, 3, 4 o 5; L es un enlace directo o -(C(R10)(R11))q-; y Cy es Ar1-B-Ar2, dondeAr1 no está presente o es un grupo arilo o heteroarilo de 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o estar mono, di o trisustituido con halógeno, alquilo inferior, alquenilo, alquinilo, cicloalquilo, -OR10, -NR10R11, -CN, -COR10 o -COOR10;B es un enlace directo, -O-, -NR10, -SO2, o -(C(R10)(R11))s-, siendo s igual a 0, 1, 2, 3, 4 o 5; yAr2 es un grupo arilo o heteroarilo de 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o estar mono, di o trisustituido con halógeno, alquilo inferior, alquenilo, alquinilo, cicloalquilo, -OR10, -NR10R11, -CN, - COR10 o -COOR10; refiriéndose alquilo, alquenilo, alquinilo, arilo o alcoxi opcionalmente sustituido a alquilo, alquenilo, arilo o alcoxi en los que opcionalmente hasta tres átomos de H de cada grupo se han sustituido por halógeno, haloalquilo, alquilo, acilo, alcoxialquilo, hidroxialquilo inferior, fenilo, heteroarilo, bencenosulfonilo, hidroxi, alcoxi inferior, haloalcoxi, carboxi, carboalcoxi (también denominado alcoxicarbonilo), alcoxicarbonilamino, carboxamido (también denominado alquilaminocarbonilo), ciano, carbonilo, acetoxi, nitro, amino, alquilamino, dialquilamino, mercapto, alquiltío, sulfóxido, sulfona, sulfonilamino, acilamino, amidino, arilo, bencilo, heterociclilo, fenoxi, benciloxi, heteroariloxi, hidroximino, alcoximino, oxalquilo, aminosulfonilo, tritilo, amidino, guanidino y ureido; y refiriéndose alquilo inferior a grupos alquilo de 1 a 6 átomos de carbono; refiriéndose alquilo a grupos alquilo C20 o menos; incluyendo cicloalquilo grupos hidrocarburo cíclicos de 3 a 8 átomos de carbono; refiriéndose los grupos alcoxi o alcoxilo a grupos de 1 a 8 átomos de carbono; refiriéndose alcoxi inferior a grupos de uno a cuatro átomos de carbono; siendo arilo y heteroarilo un anillo aromático o heteroaromático de 5 o 6 miembros que contiene 0-3 heteroátomos seleccionados entre O, N o S; un sistema de anillo aromático o heteroaromático bicíclico de 9 o 10 miembros que contiene 0-3 heteroátomos seleccionados entre O, N o S; o un sistema de anillo aromático o heteroaromático tricíclico de 13 o 14 miembros que contiene 0-3 heteroátomos seleccionados entre O, N o S; siendo uno o más anillos aromáticos sin que necesariamente tengan que serlo todos; y significando hidrocarburo C1 a C20 un grupo lineal, ramificado o cíclico formado por hidrógeno y carbono como únicos constituyentes elementales e incluyendo alquilo, cicloalquilo, policicloalquilo, alquenilo, alquinilo, arilo y combinaciones de los mismos.
Description
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Claims (1)
- -
imagen1 imagen2 imagen3 imagen4 imagen5 imagen6 imagen7 imagen8
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8225508P | 2008-07-21 | 2008-07-21 | |
| US82255P | 2008-07-21 | ||
| PCT/US2009/051200 WO2010011619A1 (en) | 2008-07-21 | 2009-07-21 | Large substituent, non-phenolic amine opioids |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2534055T3 true ES2534055T3 (es) | 2015-04-16 |
| ES2534055T9 ES2534055T9 (es) | 2016-05-31 |
Family
ID=41137538
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09790652.3T Active ES2534055T3 (es) | 2008-07-21 | 2009-07-21 | Opioides de amina no fenólicos con sustituyentes de gran tamaño |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20100190817A1 (es) |
| EP (1) | EP2318372B9 (es) |
| JP (2) | JP5727374B2 (es) |
| AU (1) | AU2009274147B2 (es) |
| CA (1) | CA2731429C (es) |
| ES (1) | ES2534055T3 (es) |
| WO (1) | WO2010011619A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100190817A1 (en) * | 2008-07-21 | 2010-07-29 | Rensselaer Polytechnic Institute | Large substituent, non-phenolic amine opioids |
| HUE043963T2 (hu) | 2009-12-04 | 2019-09-30 | Alkermes Pharma Ireland Ltd | Morfinán származékok gyógyszer-túladagolás kezelésére |
| WO2011119605A2 (en) | 2010-03-22 | 2011-09-29 | Rensselaer Polytechnic Institute | Carboxamide biosiosteres of opiates |
| EP2608670B1 (en) | 2010-08-23 | 2018-10-31 | Alkermes Pharma Ireland Limited | Methods for treating antipsychotic-induced weight gain |
| CA2840643C (en) * | 2011-06-29 | 2017-11-21 | Alkermes, Inc. | Peripherally acting opioid compounds |
| US9211293B2 (en) | 2011-12-15 | 2015-12-15 | Alkermes Pharma Ireland Limited | Opioid agonist antagonist combinations |
| US9656961B2 (en) | 2013-05-24 | 2017-05-23 | Alkermes Pharma Ireland Limited | Methods for treating depressive symptoms |
| ES2770978T3 (es) | 2013-05-24 | 2020-07-06 | Alkermes Pharma Ireland Ltd | Análogos de morfanos y morfinanos y métodos de uso |
| WO2022101444A1 (en) | 2020-11-12 | 2022-05-19 | Alkermes Pharma Ireland Limited | Immediate release multilayer tablet |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE292625T1 (de) * | 2000-10-31 | 2005-04-15 | Rensselaer Polytech Inst | 8-substituierte 2,6-methano-3-benzazocine und 3- substituierte morphinane als opioidrezeptorbindende agenzien |
| WO2004007449A1 (en) * | 2002-07-16 | 2004-01-22 | Rensselaer Polytechnic Institute | Process for conversion of phenols to carboxamides via the succinimide esters |
| AU2006272773B2 (en) * | 2005-07-21 | 2012-03-08 | Rensselaer Polytechnic Institute | 8-carboxamido-substituted-2 , 6-methano-3-benzazocines and 3 - carboxamido- substituted morphanes as opioid receptor binding agents |
| US20100190817A1 (en) * | 2008-07-21 | 2010-07-29 | Rensselaer Polytechnic Institute | Large substituent, non-phenolic amine opioids |
-
2009
- 2009-07-21 US US12/506,354 patent/US20100190817A1/en not_active Abandoned
- 2009-07-21 JP JP2011520127A patent/JP5727374B2/ja active Active
- 2009-07-21 ES ES09790652.3T patent/ES2534055T3/es active Active
- 2009-07-21 CA CA2731429A patent/CA2731429C/en active Active
- 2009-07-21 EP EP20090790652 patent/EP2318372B9/en active Active
- 2009-07-21 WO PCT/US2009/051200 patent/WO2010011619A1/en not_active Ceased
- 2009-07-21 AU AU2009274147A patent/AU2009274147B2/en not_active Ceased
-
2014
- 2014-10-03 JP JP2014204620A patent/JP2015044819A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010011619A1 (en) | 2010-01-28 |
| JP5727374B2 (ja) | 2015-06-03 |
| JP2015044819A (ja) | 2015-03-12 |
| CA2731429A1 (en) | 2010-01-28 |
| US20100190817A1 (en) | 2010-07-29 |
| EP2318372A1 (en) | 2011-05-11 |
| EP2318372B9 (en) | 2015-05-06 |
| EP2318372B1 (en) | 2015-01-14 |
| AU2009274147B2 (en) | 2014-09-04 |
| JP2011528718A (ja) | 2011-11-24 |
| CA2731429C (en) | 2016-12-13 |
| ES2534055T9 (es) | 2016-05-31 |
| AU2009274147A1 (en) | 2010-01-28 |
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