PE20090112A1 - Derivados de indol como agonistas del receptor de canabinoides cb1 - Google Patents
Derivados de indol como agonistas del receptor de canabinoides cb1Info
- Publication number
- PE20090112A1 PE20090112A1 PE2008000362A PE2008000362A PE20090112A1 PE 20090112 A1 PE20090112 A1 PE 20090112A1 PE 2008000362 A PE2008000362 A PE 2008000362A PE 2008000362 A PE2008000362 A PE 2008000362A PE 20090112 A1 PE20090112 A1 PE 20090112A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- alkyl
- tiadiazol
- tetrahydropyran
- chloro
- Prior art date
Links
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 229940054051 antipsychotic indole derivative Drugs 0.000 title 1
- BLRHMMGNCXNXJL-UHFFFAOYSA-N 1-methylindole Chemical compound C1=CC=C2N(C)C=CC2=C1 BLRHMMGNCXNXJL-UHFFFAOYSA-N 0.000 abstract 3
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 3
- -1 CARBAMOylmethyl Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4245—Oxadiazoles
-
- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
- 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
- A61P25/06—Antimigraine 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
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Otolaryngology (AREA)
- Nutrition Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
REFERIDA A UN DERIVADO DE INDOL DE FORMULA (I), DONDE A ES UN ANILLO HETEROCICLICO AROMATICO DE 5 MIEMBROS; X1, X2 Y X3 SON N, O, S O CH; Y ES CH2, O, S, SO2; R1 ES H, ALQUILO C1-C4, ALQUILOXI C1-C4, CN O HALOGENO; R2, R2', R3, R3', R4, R4', R5 Y R5' SON H, ALQUILO C1-C4 OPCIONALMENTE SUSTITUIDO CON OH, CO-OR8, ENTRE OTROS; n ES 1 O 2; R6 ES H, ALQUILO C1-C4, CO-NR9R10, CO-OR11, ENTRE OTROS; R7 ES H O HALOGENO; R8 ES ALQUILO C1-C4; R9 Y R10 SON H, ALQUILO C1-C4, CICLOALQUILO C3-C7, ENTRE OTROS; R11 ES H O ALQUILO C1-C4. SON COMPUESTOS PREFERIDOS: 3-({5-4-(CARBAMOILMETIL)-PIPERAZIN-1-IL]METIL}-[1,2,4]-TIADIAZOL-3-IL)-7-CLORO-1-(TETRAHIDROPIRAN-4-IL)METIL-1H-INDOL, 7-CLORO-3-({5-[4-(ETILCARBAMOILMETIL)PIPERAZIN-1-IL]METIL}-[1,2,4]-TIADIAZOL-3-IL)-1-(TETRAHIDROPIRAN-4-IL)METIL-1H-INDOL, 7-CLORO-3-({5-[4-(SULFAMOILPIPERAZIN-1-IL]METIL}-[1,2,4]-TIADIAZOL-3-IL)-1-(TETRAHIDROPIRAN-4-IL)METIL-1H-INDOL, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD AGONISTA DEL RECEPTOR DE CANABINOIDES CB1 Y SON UTILES EN EL TRATAMIENTO DEL DOLOR CRONICO, DOLOR NEUROPATICO, DOLOR PERIOPERATORIO, ENTRE OTROS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07102870 | 2007-02-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090112A1 true PE20090112A1 (es) | 2009-02-26 |
Family
ID=38283196
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008000362A PE20090112A1 (es) | 2007-02-22 | 2008-02-20 | Derivados de indol como agonistas del receptor de canabinoides cb1 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7655645B2 (es) |
| EP (1) | EP2125795B1 (es) |
| JP (1) | JP5324476B2 (es) |
| KR (1) | KR20090113383A (es) |
| CN (1) | CN101616914B (es) |
| AR (1) | AR065393A1 (es) |
| AU (1) | AU2008219226B2 (es) |
| BR (1) | BRPI0807867A2 (es) |
| CA (1) | CA2678147A1 (es) |
| CL (1) | CL2008000514A1 (es) |
| EC (1) | ECSP099593A (es) |
| IL (1) | IL199848A0 (es) |
| MX (1) | MX2009008316A (es) |
| PE (1) | PE20090112A1 (es) |
| RU (1) | RU2009135255A (es) |
| TW (1) | TW200848417A (es) |
| WO (1) | WO2008101995A1 (es) |
| ZA (1) | ZA200905265B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI330635B (en) | 2004-03-05 | 2010-09-21 | Organon Nv | (indol-3-yl)-heterocycle derivatives |
| US7763732B2 (en) * | 2005-08-24 | 2010-07-27 | N.V. Organon | Indole derivatives |
| TW200848417A (en) | 2007-02-22 | 2008-12-16 | Organon Nv | Indole derivatives |
| US9063126B2 (en) * | 2008-09-29 | 2015-06-23 | Abbvie Inc. | Indole and indoline derivatives and methods of use thereof |
| EP2632257B1 (en) | 2010-10-25 | 2021-03-31 | Vanderbilt University | Compositions for inhibition of insect host sensing |
| EP2704575B1 (en) | 2011-05-06 | 2020-06-03 | Vanderbilt University | Composition for inhibition of insect sensing |
| CN102757427A (zh) * | 2012-07-09 | 2012-10-31 | 陕西科技大学 | 2-氨基-5-异二氢吲哚-1,3-二酮甲基1,3,4-噻二唑及其制备方法 |
| CA3018974C (en) | 2015-03-25 | 2023-10-03 | Vanderbilt University | Binary compositions as disruptors of orco-mediated odorant sensing |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4939138A (en) * | 1988-12-29 | 1990-07-03 | Sterling Drug Inc. | 2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo(1,2,3-DE)-1,4-benzoxazines |
| TWI292316B (en) * | 1999-10-11 | 2008-01-11 | Sod Conseils Rech Applic | Pharmaceutical composition of thiazole derivatives intended to inhibit mao and/or lipidic peroxidation and/or to act as modulators of sodium channels and the use thereof |
| WO2001058869A2 (en) | 2000-02-11 | 2001-08-16 | Bristol-Myers Squibb Company | Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases |
| AUPR118000A0 (en) | 2000-11-02 | 2000-11-23 | Amrad Operations Pty. Limited | Therapeutic molecules and methods |
| EP1363632B1 (en) | 2001-01-29 | 2010-08-25 | The University of Connecticut | Receptor selective cannabimimetic aminoalkylindoles |
| TWI248438B (en) * | 2001-04-10 | 2006-02-01 | Sod Conseils Rech Applic | Derivatives of heterocycles with 5 members, their preparation and their use as medicaments |
| TW200402417A (en) | 2002-06-21 | 2004-02-16 | Akzo Nobel Nv | 1-[(Indol-3-yl)carbonyl]piperazine derivatives |
| BRPI0417626A (pt) | 2003-12-17 | 2007-03-27 | Akzo Nobel Nv | derivado de 1-[(indol-3-il) carbonil] piperazina tricìclica, composição farmacêutica, uso de um derivado de 1-[(indol-3-il) carbonil] piperazina tricìclica |
| TWI330635B (en) | 2004-03-05 | 2010-09-21 | Organon Nv | (indol-3-yl)-heterocycle derivatives |
| EP1904068A1 (en) * | 2005-07-11 | 2008-04-02 | N.V. Organon | Synergistic combination for the treatment of pain (cannabioid receptor agonist and opiod receptor agonist) |
| TW200745096A (en) | 2005-08-23 | 2007-12-16 | Organon Nv | Indole derivatives |
| US7763732B2 (en) * | 2005-08-24 | 2010-07-27 | N.V. Organon | Indole derivatives |
| TW200848417A (en) | 2007-02-22 | 2008-12-16 | Organon Nv | Indole derivatives |
-
2008
- 2008-01-29 TW TW097103332A patent/TW200848417A/zh unknown
- 2008-02-15 US US12/031,851 patent/US7655645B2/en not_active Expired - Fee Related
- 2008-02-20 AR ARP080100681A patent/AR065393A1/es unknown
- 2008-02-20 PE PE2008000362A patent/PE20090112A1/es not_active Application Discontinuation
- 2008-02-20 CL CL200800514A patent/CL2008000514A1/es unknown
- 2008-02-21 RU RU2009135255/04A patent/RU2009135255A/ru not_active Application Discontinuation
- 2008-02-21 JP JP2009550715A patent/JP5324476B2/ja not_active Expired - Fee Related
- 2008-02-21 CA CA002678147A patent/CA2678147A1/en not_active Abandoned
- 2008-02-21 WO PCT/EP2008/052141 patent/WO2008101995A1/en not_active Ceased
- 2008-02-21 KR KR1020097019668A patent/KR20090113383A/ko not_active Withdrawn
- 2008-02-21 EP EP08709170A patent/EP2125795B1/en active Active
- 2008-02-21 MX MX2009008316A patent/MX2009008316A/es active IP Right Grant
- 2008-02-21 CN CN2008800057712A patent/CN101616914B/zh not_active Expired - Fee Related
- 2008-02-21 AU AU2008219226A patent/AU2008219226B2/en not_active Ceased
- 2008-02-21 BR BRPI0807867-0A2A patent/BRPI0807867A2/pt not_active IP Right Cessation
-
2009
- 2009-07-14 IL IL199848A patent/IL199848A0/en unknown
- 2009-07-28 ZA ZA200905265A patent/ZA200905265B/xx unknown
- 2009-08-21 EC EC2009009593A patent/ECSP099593A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2010519278A (ja) | 2010-06-03 |
| US20080207598A1 (en) | 2008-08-28 |
| EP2125795A1 (en) | 2009-12-02 |
| AR065393A1 (es) | 2009-06-03 |
| CN101616914B (zh) | 2012-10-10 |
| IL199848A0 (en) | 2010-04-15 |
| CN101616914A (zh) | 2009-12-30 |
| JP5324476B2 (ja) | 2013-10-23 |
| ECSP099593A (es) | 2009-09-29 |
| CL2008000514A1 (es) | 2008-06-20 |
| WO2008101995A1 (en) | 2008-08-28 |
| EP2125795B1 (en) | 2013-03-20 |
| AU2008219226A1 (en) | 2008-08-28 |
| BRPI0807867A2 (pt) | 2014-06-03 |
| ZA200905265B (en) | 2010-04-28 |
| CA2678147A1 (en) | 2008-08-28 |
| RU2009135255A (ru) | 2011-03-27 |
| AU2008219226B2 (en) | 2013-02-07 |
| US7655645B2 (en) | 2010-02-02 |
| MX2009008316A (es) | 2009-08-12 |
| TW200848417A (en) | 2008-12-16 |
| KR20090113383A (ko) | 2009-10-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |