ES2653265T3 - Morfinanos sustituidos y el uso de éstos - Google Patents
Morfinanos sustituidos y el uso de éstos Download PDFInfo
- Publication number
- ES2653265T3 ES2653265T3 ES13823996T ES13823996T ES2653265T3 ES 2653265 T3 ES2653265 T3 ES 2653265T3 ES 13823996 T ES13823996 T ES 13823996T ES 13823996 T ES13823996 T ES 13823996T ES 2653265 T3 ES2653265 T3 ES 2653265T3
- Authority
- ES
- Spain
- Prior art keywords
- cycloalkyl
- cycloalkenyl
- heterocycle
- alkyl
- heteroaryl
- 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
- 150000003810 morphinanes Chemical class 0.000 title 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 9
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 125000001475 halogen functional group Chemical group 0.000 abstract 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 4
- 125000003282 alkyl amino group Chemical group 0.000 abstract 4
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- -1 cyano, carboxy Chemical group 0.000 abstract 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P1/10—Laxatives
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- 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
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D215/14—Radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto que tiene la Fórmula I-A: **(Ver fórmula)** o una sal o solvato farmacéuticamente aceptable de éste, en el que: R1 es hidrógeno, OH, halo, ciano, carboxi, o aminocarbonilo; o alquilo, alquenilo, alquinilo, alcoxi, alqueniloxi, o alquiniloxi, cualquiera de los cuales está sustituido opcionalmente con 1, 2, ó 3 sustituyentes, cada uno seleccionado independientemente del grupo que consiste en hidroxi, halo, haloalquilo, amino, alquilamino, dialquilamino, carboxi, alcoxi, alcoxicarbonilo, arilo, heteroarilo, heterociclo, cicloalquilo, y cicloalquenilo, en el que el arilo, heteroarilo, heterociclo, cicloalquilo, y cicloalquenilo están sustituidos opcionalmente con 1, 2, ó 3 grupos R11a seleccionados independientemente; R2 es: (a) hidrógeno o carboxamido; o (b) alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, heterociclo, arilo, heteroarilo, (cicloalquil)alquilo, (cicloalquenil)alquilo, (heterociclo)alquilo, arilalquilo, heteroarilalquilo, alquilcarbonilo, alcoxicarbonilo, (arilalcoxi)carbonilo, o (heteroarilalcoxi)carbonilo, cualquiera de los cuales está sustituido opcionalmente con 1, 2, ó 3 sustituyentes, cada uno seleccionado independientemente del grupo que consiste en hidroxi, alquilo, halo, haloalquilo, amino, alquilamino, dialquilamino, carboxi, alcoxi, alcoxicarbonilo, arilo, heteroarilo, heterociclo, cicloalquilo, y cicloalquenilo, en el que el arilo, heteroarilo, heterociclo, cicloalquilo, y cicloalquenilo están sustituidos opcionalmente con 1, 2, ó 3 grupos R11a seleccionados independientemente; R3 es hidrógeno, OH, o halo; o alcoxi, alquilamino, o dialquilamino, cualquiera de los cuales está sustituido opcionalmente con 1, 2, ó 3 sustituyentes, cada uno seleccionado independientemente del grupo que consiste en hidroxilo, halo, haloalquilo, amino, alquilamino, dialquilamino, carboxi, alcoxi, alcoxicarbonilo, arilo, heteroarilo, heterociclo, cicloalquilo, y cicloalquenilo, en el que el arilo, heteroarilo, heterociclo, cicloalquilo, y cicloalquenilo están sustituidos opcionalmente con 1, 2, ó 3 grupos R11a seleccionados independientemente; R4a1 se selecciona del grupo que consiste en alquilo C3-C6, arilalquilo, (cicloalquil)alquilo, alcoxi C3-C6, aralquiloxi, -N(H)COR4c, -CH2C(>=O)NR4dR4e, -N(H)SO2R4f, **(Ver fórmula)** ...
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261746878P | 2012-12-28 | 2012-12-28 | |
| PCT/IB2013/002883 WO2014102593A1 (en) | 2012-12-28 | 2013-12-23 | Substituted morphinans and the use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2653265T3 true ES2653265T3 (es) | 2018-02-06 |
Family
ID=50000021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13823996T Active ES2653265T3 (es) | 2012-12-28 | 2013-12-23 | Morfinanos sustituidos y el uso de éstos |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8946255B2 (es) |
| EP (1) | EP2941431B1 (es) |
| JP (1) | JP6159417B2 (es) |
| AR (1) | AR094646A1 (es) |
| CA (1) | CA2896202A1 (es) |
| ES (1) | ES2653265T3 (es) |
| IL (1) | IL239643A0 (es) |
| TW (1) | TW201441199A (es) |
| WO (1) | WO2014102593A1 (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2013003354A (es) | 2010-09-21 | 2013-06-24 | Purdue Pharma Lp | Analogos de buprenorfina. |
| EP3333156A3 (en) | 2012-11-09 | 2018-09-26 | Purdue Pharma L.P. | Benzomorphan analogs and the use thereof |
| US9175000B2 (en) | 2012-12-07 | 2015-11-03 | Purdue Pharma L.P. | Buprenorphine analogs |
| WO2014091297A1 (en) | 2012-12-14 | 2014-06-19 | Purdue Pharma L.P. | Spirocyclic morphinans and their use |
| TWI513697B (zh) | 2012-12-14 | 2015-12-21 | Purdue Pharma Lp | 吡啶酮並嗎啡喃類似物及其對類鴉片受體之生物活性 |
| US9056836B2 (en) | 2013-01-31 | 2015-06-16 | Purdue Pharma L.P. | Benzomorphan analogs and the use thereof |
| US8969358B2 (en) | 2013-03-15 | 2015-03-03 | Purdue Pharma L.P. | Buprenorphine analogs |
| EP3087073B1 (en) | 2013-12-26 | 2018-07-04 | Purdue Pharma LP | 10-substituted morphinan hydantoins |
| AU2014370062A1 (en) | 2013-12-26 | 2016-08-11 | Purdue Pharma L.P. | Ring-contracted morphinans and the use thereof |
| EP3087078B1 (en) | 2013-12-26 | 2019-05-15 | Purdue Pharma LP | 7-beta-alkyl analogs of orvinols |
| EP3087079B1 (en) | 2013-12-26 | 2019-04-03 | Purdue Pharma LP | Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans |
| WO2015097546A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | Propellane-based compounds and their use as opioid receptor modulators |
| US10550088B2 (en) | 2013-12-27 | 2020-02-04 | Purdue Pharma L.P. | 6-substituted and 7-substituted morphinan analogs and the use thereof |
| JP2017521373A (ja) | 2014-05-27 | 2017-08-03 | パーデュー、ファーマ、リミテッド、パートナーシップ | スピロ環モルフィナン及びその使用 |
| EP3154972A4 (en) | 2014-06-13 | 2017-11-22 | Purdue Pharma L.P. | Azamophinan derivatives and use thereof |
| MA41125A (fr) | 2014-12-05 | 2017-10-10 | Purdue Pharma Lp | Dérivés de 6.7-cyclomorphinane et leur utilisation |
| MD3344248T2 (ro) * | 2015-09-02 | 2022-10-31 | Trevena Inc | Aza-heterociclic cu 6 elemente conținând compuși de modulare a receptorului delta-opioid, metode de utilizare și fabricare a acestora |
| US10745402B2 (en) | 2017-01-02 | 2020-08-18 | Purdue Pharma L.P. | Morphinan derivatives and use thereof |
| GB201719667D0 (en) * | 2017-11-27 | 2018-01-10 | Johnson Matthey Plc | Process |
| WO2021015109A1 (ja) | 2019-07-19 | 2021-01-28 | 日本ケミファ株式会社 | フェノール誘導体の製造方法 |
| AR125188A1 (es) | 2021-03-22 | 2023-06-21 | Neurocrine Biosciences Inc | Inhibidores del vmat2 y métodos de uso |
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| US8987293B2 (en) * | 2010-12-23 | 2015-03-24 | Phoenix Pharmalabs, Inc. | Morphinans useful as analgesics |
| ES2629185T3 (es) | 2011-08-26 | 2017-08-07 | Deutsche Diabetes-Forschungsgesellschaft e. V. | Derivados de morfinano para el tratamiento de la diabetes y trastornos relacionados |
| JP6061857B2 (ja) | 2011-09-09 | 2017-01-18 | 学校法人北里研究所 | モルヒナン誘導体 |
| US8937084B2 (en) | 2012-12-14 | 2015-01-20 | Purdue Pharma L.P. | Nitrogen containing morphinan derivatives and the use thereof |
-
2013
- 2013-12-23 US US14/138,691 patent/US8946255B2/en active Active - Reinstated
- 2013-12-23 EP EP13823996.7A patent/EP2941431B1/en active Active
- 2013-12-23 JP JP2015550154A patent/JP6159417B2/ja not_active Expired - Fee Related
- 2013-12-23 WO PCT/IB2013/002883 patent/WO2014102593A1/en not_active Ceased
- 2013-12-23 ES ES13823996T patent/ES2653265T3/es active Active
- 2013-12-23 TW TW102147764A patent/TW201441199A/zh unknown
- 2013-12-23 CA CA2896202A patent/CA2896202A1/en not_active Abandoned
- 2013-12-27 AR ARP130105048A patent/AR094646A1/es unknown
-
2014
- 2014-12-19 US US14/576,718 patent/US9388162B2/en active Active
-
2015
- 2015-06-25 IL IL239643A patent/IL239643A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL239643A0 (en) | 2015-08-31 |
| US8946255B2 (en) | 2015-02-03 |
| JP6159417B2 (ja) | 2017-07-05 |
| AR094646A1 (es) | 2015-08-19 |
| WO2014102593A1 (en) | 2014-07-03 |
| TW201441199A (zh) | 2014-11-01 |
| US20150175571A1 (en) | 2015-06-25 |
| CA2896202A1 (en) | 2014-07-03 |
| JP2016509588A (ja) | 2016-03-31 |
| US20140187573A1 (en) | 2014-07-03 |
| US9388162B2 (en) | 2016-07-12 |
| EP2941431A1 (en) | 2015-11-11 |
| EP2941431B1 (en) | 2017-10-25 |
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