AR077991A1 - Moduladores del receptor de cannabinoides - Google Patents
Moduladores del receptor de cannabinoidesInfo
- Publication number
- AR077991A1 AR077991A1 ARP100103145A ARP100103145A AR077991A1 AR 077991 A1 AR077991 A1 AR 077991A1 AR P100103145 A ARP100103145 A AR P100103145A AR P100103145 A ARP100103145 A AR P100103145A AR 077991 A1 AR077991 A1 AR 077991A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- cycloalkyl
- aryl
- heteroaryl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
Abstract
La presente se refiere a ciertos compuestos y composiciones farmacéuticas de los mismos que modulan la actividad del receptor de cannabinoides CB2. La presente adicionalmente se refiere a ciertos compuestos y composiciones farmacéuticas de los mismos que modulan las actividades del receptor CB1 y del receptor CB2. Los compuestos de la presente y composiciones farmacéuticas de los mismos se dirigen a métodos utiles en el tratamiento de: dolor, por ejemplo dolor oseo y articular, dolor muscular, dolor dental, migrana y otro dolor de cabeza, dolor inflamatorio, dolor neuropático, dolor que se produce como un efecto adverso de un tratamiento médico y dolor asociado con osteoartritis; hiperalgesia; alodinia; hiperalgesia inflamatoria; hiperalgesia neuropática; nocicepcion aguda; osteoporosis; espasticidad asociada a la esclerosis multiple; trastornos autoinmunes; reacciones alérgicas; inflamacion del SNC; aterosclerosis; actividad celular inmune no deseada e inflamacion; degeneracion macular asociada con la edad; tos; leucemia; linfoma; tumores del SNC; cáncer de prostata; enfermedad de Alzheimer; dano inducido por accidente cerebrovascular; demencia; esclerosis lateral amiotrofica y enfermedad de Parkinson. Reivindicacion 1: Un compuesto que se selecciona de compuestos de Formula 1a y sales, solvatos, hidratos y N-oxidos farmacéuticamente aceptables de los mismos: en donde: R1, R2, R3, R4, R5 y R6 se seleccionan, cada uno, independientemente de: H y alquilo C1-6 X es NR7 e Y es CC(O)N(R8)R9 o X es CC(O)N(R8)R9 e Y es NR7; R7 es -R10-R11-R12-R13 en donde: R10 se selecciona de: alquileno C1-6, heteroarileno y heterociclileno; o R10 está ausente; R11 se selecciona de: -C(O)NH- y alquileno C1-6 o R11 está ausente; R12 es alquileno C1-6 o R12 está ausente; y R13 se selecciona de: alquilo C1-6, arilo, cicloalquilo C3-7, heteroarilo, heterociclilo e hidroxilo; en donde dichos alquilo C1-6, arilo y heteroarilo se sustituyen, cada uno, opcionalmente por uno o dos sustituyentes que se seleccionan de: alcoxi C1-6, alquilo C1-6, alquil C1-6 amino, alquilsulfonilo C1-6, amino, cicloalquilo C3-7, ciano, dialquil C2-8 amino, haloalquilo C1-6, halogeno e hidroxilo; R8 es -R14-R15-R16-R17 en donde: R14 se selecciona de: alquileno C1-6, cicloalquenileno C3-7, cicloalquileno C3-7, heteroarileno y heterociclileno; en donde dichos alquileno C1-6 y heterociclileno se sustituyen, cada uno, opcionalmente por uno o más sustituyentes que se seleccionan de: alcoxi C1-6 carbonilo, alquilo C1-6, cicloalquilo C3-7, arilo, carboxi, heteroarilo, heterociclilo e hidroxilo; en donde dichos alquilo C1-6 y arilo se sustituyen opcionalmente por un sustituyente que se selecciona de: alcoxi C1-6, arilo, halogeno, heteroarilo e hidroxilo; o R14 está ausente; R15 se selecciona de: -C(O)NH-, -C(O)-, -C(O)O-, alquileno C1-6, cicloalquileno C3-7, heteroarileno y heterociclileno; en donde dicho heterociclileno se sustituye opcionalmente por alquilo C1-6 o R15 está ausente; R16 es alquileno C1-6 o R16 está ausente; y R17 se selecciona de: H, alcoxi C1-6, alquilo C1-6, alquil C1-6 amino, alquil C1-6 carboxamida, alquinilo C2-6, ureilo, amino, arilo, arilamino, arilcarbonilo, ariloxi, carboalcoxi C1-6, carboxamida, carboxi, ciano, cicloalquilo C3-7, bicicloalquilo C5-11, cicloalquil C3-7 amino, dialquil C2-8 amino, dialquil C2-8 sulfonamida, haloalquilo C1-6, heteroarilo, heteroariloxi, heterobiciclilo, heterociclilo, hidroxilo y fosfonooxi; en donde dichos alquil C1-6 amino, amino, arilo, arilamino, ariloxi, bicicloalquilo C5-11, cicloalquilo C3-7, cicloalquil C3-7 amino, heteroarilo, heterobiciclilo, heterociclilo y ureilo se sustituyen, cada uno, opcionalmente por uno o más sustituyentes que se seleccionan de: alcoxi C1-6, alcoxi C1-6 carbonilo, alquilo C1-6, alquilsulfonilo C1-6, amino, arilo, carboxi, ciano, cicloalquilo C3-7, dialquil C2-8 amino, haloalcoxi C1-6, haloalquilo C1-6, halogeno, heteroarilo, heterociclilo e hidroxilo; y R9 se selecciona de H, alquilo C1-6 y cicloalquilo C3-7 o R8 y R9 junto con el átomo de nitrogeno al que están unidos forman un grupo que se selecciona de: heterociclilo y heterobiciclilo, cada uno opcionalmente sustituido por uno o más sustituyentes que se seleccionan de: carboalcoxi C1-6, alcoxi C1-6, alquilo C1-6, arilo, carboalcoxi C1-6, haloalquilo C1-6, halogeno, heteroarilo, heteroariloxi, heterociclilo e hidroxilo; en donde dichos arilo, alquilo C1-6 y heteroarilo se sustituyen opcionalmente por un sustituyente que se selecciona de: cicloalquilo C3-7, alcoxi C1-6, halogeno e hidroxilo.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27550609P | 2009-08-28 | 2009-08-28 | |
| US39658810P | 2010-05-28 | 2010-05-28 | |
| US40014610P | 2010-07-22 | 2010-07-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077991A1 true AR077991A1 (es) | 2011-10-05 |
Family
ID=43127457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103145A AR077991A1 (es) | 2009-08-28 | 2010-08-27 | Moduladores del receptor de cannabinoides |
Country Status (19)
| Country | Link |
|---|---|
| US (6) | US8778950B2 (es) |
| EP (4) | EP4036082A1 (es) |
| JP (5) | JP5746698B2 (es) |
| KR (6) | KR20180115807A (es) |
| CN (2) | CN102596913B (es) |
| AR (1) | AR077991A1 (es) |
| AU (1) | AU2010286988B2 (es) |
| BR (1) | BR112012008159A2 (es) |
| CA (1) | CA2770866C (es) |
| EA (1) | EA023586B1 (es) |
| HK (1) | HK1259082A1 (es) |
| IL (1) | IL218130A (es) |
| IN (1) | IN2012DN02474A (es) |
| MX (1) | MX2012002499A (es) |
| NZ (1) | NZ598288A (es) |
| SG (3) | SG178907A1 (es) |
| TW (1) | TWI503316B (es) |
| WO (1) | WO2011025541A1 (es) |
| ZA (1) | ZA202205142B (es) |
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|---|---|---|---|---|
| IN2012DN02474A (es) * | 2009-08-28 | 2015-08-21 | Arena Pharm Inc | |
| US9597340B2 (en) * | 2011-02-25 | 2017-03-21 | Arena Pharmaceuticals, Inc. | Cannabinoid receptor modulators |
| JP5945554B2 (ja) | 2011-02-25 | 2016-07-05 | アリーナ ファーマシューティカルズ， インコーポレイテッド | 縮合型アザ環の結晶形およびその調製プロセス（カンナビノイド受容体モジュレーター） |
| US20140206649A1 (en) * | 2011-02-25 | 2014-07-24 | Jayant Thatte | Cannabinoid receptor modulators |
| ITMI20122221A1 (it) | 2012-12-21 | 2014-06-22 | C4T S C A R L | Nuovi composti del 2,3-diidro-4h-1,3-benzossazin-4-one, metodo per prepararli e forma farmaceutica che li comprende |
| EP2803668A1 (en) | 2013-05-17 | 2014-11-19 | Boehringer Ingelheim International Gmbh | Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles |
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| EA201992638A1 (ru) * | 2017-05-08 | 2020-03-18 | Арена Фармасьютикалз, Инк. | Соединения и способы для лечения висцеральной боли |
| WO2018208847A1 (en) | 2017-05-08 | 2018-11-15 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of pain from inflammatory bowel disease |
| WO2019043635A1 (en) | 2017-09-01 | 2019-03-07 | Richter Gedeon Nyrt. | COMPOUNDS INHIBITING THE ACTIVITY OF D-AMINO ACID OXIDASE |
| US20230008022A1 (en) * | 2018-11-28 | 2023-01-12 | Merck Sharp & Dohme Corp. | Novel substituted piperazine amide compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
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