ECSP12012347A - Derivados de amino-tropano - Google Patents
Derivados de amino-tropanoInfo
- Publication number
- ECSP12012347A ECSP12012347A ECSP12012347A ECSP12012347A EC SP12012347 A ECSP12012347 A EC SP12012347A EC SP12012347 A ECSP12012347 A EC SP12012347A EC SP12012347 A ECSP12012347 A EC SP12012347A
- Authority
- EC
- Ecuador
- Prior art keywords
- lower alkyl
- glyt
- compounds
- inhibitors
- amino
- Prior art date
Links
- FHPZUVVXVRYZAS-SFYZADRCSA-N (1r,5s)-8-methyl-8-azabicyclo[3.2.1]octan-5-amine Chemical class C1CC[C@@]2(N)CC[C@]1([H])N2C FHPZUVVXVRYZAS-SFYZADRCSA-N 0.000 title 1
- 102000010726 Glycine Plasma Membrane Transport Proteins Human genes 0.000 abstract 4
- 108010063380 Glycine Plasma Membrane Transport Proteins Proteins 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención, se refiere a compuestos de la fórmula general I en donde, R1, R2 y R3, son, de una forma independiente la una con respecto a la otra, hidrógeno, alquilo inferior, alcoxi inferior, cicloalquilo, alquilo inferior sustituido por halógeno, ó S-alquilo inferior;o a sales de adición de ácidos, farmacéuticamente aceptables, a una mezcla racémica, o sus correspondientes enantiómeros y / o isómeros ópticos de ésta.Se ha encontrado el hecho de que, los compuestos de las fórmulas generales I, son buenos inhibidores del transportador de glicina 1 (GlyT-1), y que éstos tienen una buena selectividad a los inhibidores del transportador de glicina 2 (GlyT-2), apropiados en el tratamiento de los trastornos neurológicos y neuropsiquiátricos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10166757 | 2010-06-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP12012347A true ECSP12012347A (es) | 2013-01-31 |
Family
ID=44310862
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP12012347 ECSP12012347A (es) | 2010-06-22 | 2012-12-20 | Derivados de amino-tropano |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8153653B2 (es) |
| EP (1) | EP2585456B1 (es) |
| JP (1) | JP5546684B2 (es) |
| KR (1) | KR101445016B1 (es) |
| CN (1) | CN102947297B (es) |
| AR (1) | AR081961A1 (es) |
| AU (1) | AU2011269145A1 (es) |
| BR (1) | BR112012032576A2 (es) |
| CA (1) | CA2801458C (es) |
| CL (1) | CL2012003552A1 (es) |
| CO (1) | CO6630160A2 (es) |
| CR (1) | CR20120614A (es) |
| EA (1) | EA201291374A1 (es) |
| EC (1) | ECSP12012347A (es) |
| ES (1) | ES2550831T3 (es) |
| IL (1) | IL222998A0 (es) |
| MA (1) | MA34251B1 (es) |
| MX (1) | MX2012013820A (es) |
| PE (1) | PE20130317A1 (es) |
| PH (1) | PH12012502339A1 (es) |
| SG (1) | SG186329A1 (es) |
| TW (1) | TWI417097B (es) |
| WO (1) | WO2011161006A1 (es) |
| ZA (1) | ZA201209248B (es) |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG99853A1 (en) * | 1996-02-22 | 2003-11-27 | Neurosearch As | Tropane-derivatives, their preparation and use |
| US5834484A (en) * | 1997-03-12 | 1998-11-10 | Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Cocaine analogs |
| CA2537292C (en) * | 2003-09-09 | 2013-04-02 | F. Hoffmann-La Roche Ag | 1- (2-amino-benzol) -piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses |
| FR2861076B1 (fr) | 2003-10-17 | 2006-01-06 | Sanofi Synthelabo | Derives de n-heterocyclymethylbenzamide, leur preparation et leur application en therapeutique |
| US7572792B2 (en) * | 2004-04-29 | 2009-08-11 | Merck & Co., Inc. | Azetidine glycine transporter inhibitors |
| FR2873693B1 (fr) * | 2004-07-29 | 2006-09-15 | Sanofi Synthelabo | Derives d'amino-tropane, leur preparation et leur application en therapeutique |
| GB0428231D0 (en) * | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Compounds |
| CA2593453A1 (en) * | 2005-01-06 | 2006-07-13 | F. Hoffmann-La Roche Ag | Sulfanyl substituted phenyl methanones as glycine transporter 1 (glyt-1) inhibitors for the treatment of neurological and neuropsychiatric disorders |
| TW200846328A (en) * | 2007-02-01 | 2008-12-01 | Glaxo Group Ltd | GlyT1 transporter inhibitors and uses thereof in treatment of neurological and neuropsychiatric disorders |
| WO2010020548A1 (en) * | 2008-08-20 | 2010-02-25 | F. Hoffmann-La Roche Ag | Glyt1 receptor antagonists |
-
2011
- 2011-06-15 US US13/160,559 patent/US8153653B2/en not_active Expired - Fee Related
- 2011-06-17 PH PH1/2012/502339A patent/PH12012502339A1/en unknown
- 2011-06-17 JP JP2013515816A patent/JP5546684B2/ja not_active Expired - Fee Related
- 2011-06-17 MA MA35398A patent/MA34251B1/fr unknown
- 2011-06-17 SG SG2012091708A patent/SG186329A1/en unknown
- 2011-06-17 PE PE2012002444A patent/PE20130317A1/es not_active Application Discontinuation
- 2011-06-17 CA CA2801458A patent/CA2801458C/en not_active Expired - Fee Related
- 2011-06-17 EP EP11728224.4A patent/EP2585456B1/en active Active
- 2011-06-17 CN CN201180030703.3A patent/CN102947297B/zh not_active Expired - Fee Related
- 2011-06-17 BR BR112012032576A patent/BR112012032576A2/pt active Search and Examination
- 2011-06-17 MX MX2012013820A patent/MX2012013820A/es active IP Right Grant
- 2011-06-17 WO PCT/EP2011/060073 patent/WO2011161006A1/en not_active Ceased
- 2011-06-17 KR KR1020127033182A patent/KR101445016B1/ko not_active Expired - Fee Related
- 2011-06-17 ES ES11728224.4T patent/ES2550831T3/es active Active
- 2011-06-17 AU AU2011269145A patent/AU2011269145A1/en not_active Abandoned
- 2011-06-17 EA EA201291374A patent/EA201291374A1/ru unknown
- 2011-06-20 TW TW100121503A patent/TWI417097B/zh not_active IP Right Cessation
- 2011-06-21 AR ARP110102138A patent/AR081961A1/es unknown
-
2012
- 2012-10-26 CO CO12192372A patent/CO6630160A2/es active IP Right Grant
- 2012-11-12 IL IL222998A patent/IL222998A0/en unknown
- 2012-12-05 CR CR20120614A patent/CR20120614A/es unknown
- 2012-12-06 ZA ZA2012/09248A patent/ZA201209248B/en unknown
- 2012-12-17 CL CL2012003552A patent/CL2012003552A1/es unknown
- 2012-12-20 EC ECSP12012347 patent/ECSP12012347A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SG186329A1 (en) | 2013-01-30 |
| EP2585456A1 (en) | 2013-05-01 |
| AR081961A1 (es) | 2012-10-31 |
| CN102947297A (zh) | 2013-02-27 |
| CR20120614A (es) | 2013-01-11 |
| EA201291374A1 (ru) | 2013-06-28 |
| EP2585456B1 (en) | 2015-09-16 |
| BR112012032576A2 (pt) | 2016-11-22 |
| HK1179606A1 (zh) | 2013-10-04 |
| MA34251B1 (fr) | 2013-05-02 |
| PH12012502339A1 (en) | 2013-02-11 |
| CN102947297B (zh) | 2015-12-16 |
| PE20130317A1 (es) | 2013-03-11 |
| ES2550831T3 (es) | 2015-11-12 |
| US8153653B2 (en) | 2012-04-10 |
| WO2011161006A1 (en) | 2011-12-29 |
| AU2011269145A1 (en) | 2012-11-08 |
| KR101445016B1 (ko) | 2014-09-26 |
| KR20130029414A (ko) | 2013-03-22 |
| ZA201209248B (en) | 2013-08-28 |
| TWI417097B (zh) | 2013-12-01 |
| CA2801458C (en) | 2018-10-30 |
| JP2013529607A (ja) | 2013-07-22 |
| TW201206438A (en) | 2012-02-16 |
| MX2012013820A (es) | 2013-01-28 |
| IL222998A0 (en) | 2013-02-03 |
| CL2012003552A1 (es) | 2013-04-12 |
| US20110312993A1 (en) | 2011-12-22 |
| CA2801458A1 (en) | 2011-12-29 |
| CO6630160A2 (es) | 2013-03-01 |
| JP5546684B2 (ja) | 2014-07-09 |
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