PE20220137A1 - Moduladores del receptor de nmda - Google Patents
Moduladores del receptor de nmdaInfo
- Publication number
- PE20220137A1 PE20220137A1 PE2021002225A PE2021002225A PE20220137A1 PE 20220137 A1 PE20220137 A1 PE 20220137A1 PE 2021002225 A PE2021002225 A PE 2021002225A PE 2021002225 A PE2021002225 A PE 2021002225A PE 20220137 A1 PE20220137 A1 PE 20220137A1
- Authority
- PE
- Peru
- Prior art keywords
- amino
- alkyl
- hydrogen
- haloalkyl
- cycloalkyl
- Prior art date
Links
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 title abstract 2
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 title abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
- ASWNPURWTQJVQD-ZCFIWIBFSA-N N[C@@H](C(=O)O)CNC(=O)C1=CC2=NC=CC(=C2S1)C(F)F Chemical compound N[C@@H](C(=O)O)CNC(=O)C1=CC2=NC=CC(=C2S1)C(F)F ASWNPURWTQJVQD-ZCFIWIBFSA-N 0.000 abstract 1
- ZHCRQYOPNJVNTH-SECBINFHSA-N N[C@@H](C(=O)O)CNC(=O)C1=CC2=NC=CC(=C2S1)C1CC1 Chemical compound N[C@@H](C(=O)O)CNC(=O)C1=CC2=NC=CC(=C2S1)C1CC1 ZHCRQYOPNJVNTH-SECBINFHSA-N 0.000 abstract 1
- VWRBMYVRTNAYKU-MRVPVSSYSA-N N[C@@H](C(=O)O)CNC(=O)C1=CC2=NC=CC(=C2S1)CC Chemical compound N[C@@H](C(=O)O)CNC(=O)C1=CC2=NC=CC(=C2S1)CC VWRBMYVRTNAYKU-MRVPVSSYSA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 235000019260 propionic acid Nutrition 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B62—LAND VEHICLES FOR TRAVELLING OTHERWISE THAN ON RAILS
- B62D—MOTOR VEHICLES; TRAILERS
- B62D15/00—Steering not otherwise provided for
- B62D15/02—Steering position indicators ; Steering position determination; Steering aids
- B62D15/027—Parking aids, e.g. instruction means
- B62D15/0285—Parking performed automatically
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P25/24—Antidepressants
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B60—VEHICLES IN GENERAL
- B60W—CONJOINT CONTROL OF VEHICLE SUB-UNITS OF DIFFERENT TYPE OR DIFFERENT FUNCTION; CONTROL SYSTEMS SPECIALLY ADAPTED FOR HYBRID VEHICLES; ROAD VEHICLE DRIVE CONTROL SYSTEMS FOR PURPOSES NOT RELATED TO THE CONTROL OF A PARTICULAR SUB-UNIT
- B60W30/00—Purposes of road vehicle drive control systems not related to the control of a particular sub-unit, e.g. of systems using conjoint control of vehicle sub-units
- B60W30/06—Automatic manoeuvring for parking
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B60—VEHICLES IN GENERAL
- B60W—CONJOINT CONTROL OF VEHICLE SUB-UNITS OF DIFFERENT TYPE OR DIFFERENT FUNCTION; CONTROL SYSTEMS SPECIALLY ADAPTED FOR HYBRID VEHICLES; ROAD VEHICLE DRIVE CONTROL SYSTEMS FOR PURPOSES NOT RELATED TO THE CONTROL OF A PARTICULAR SUB-UNIT
- B60W60/00—Drive control systems specially adapted for autonomous road vehicles
- B60W60/001—Planning or execution of driving tasks
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B60—VEHICLES IN GENERAL
- B60W—CONJOINT CONTROL OF VEHICLE SUB-UNITS OF DIFFERENT TYPE OR DIFFERENT FUNCTION; CONTROL SYSTEMS SPECIALLY ADAPTED FOR HYBRID VEHICLES; ROAD VEHICLE DRIVE CONTROL SYSTEMS FOR PURPOSES NOT RELATED TO THE CONTROL OF A PARTICULAR SUB-UNIT
- B60W2510/00—Input parameters relating to a particular sub-units
- B60W2510/20—Steering systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Mechanical Engineering (AREA)
- Transportation (AREA)
- Automation & Control Theory (AREA)
- Epidemiology (AREA)
- Human Computer Interaction (AREA)
- Combustion & Propulsion (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Referida a un compuesto de Formula I, o una sal farmaceuticamente aceptable del mismo, donde R1 es hidrogeno, halogeno, haloalquilo C1-4, ciano, cicloalquilo C3-6 y alquilo C1-4; R2 es hidrogeno, halogeno, haloalquilo C1-4, ciano, 15 cicloalquilo C3-6, y alquilo C1-4; R3 es hidrogeno, halogeno, haloalquilo C1-4, ciano, cicloalquilo C3-6, y alquilo C1-4; R4 es hidrogeno, halogeno, alquilo C1-4, haloalquilo C1-4, hidroxialquilo C1-4, hidroxihaloalquilo C1-4, ciano, NRaRb , SRcRd , OR6 , L-(OR6 ) y R7; Ra y Rb son hidrogeno y alquilo C1-4; Rc y Rd son hidrogeno y alquilo C1-4; R6 es hidrogeno, alquilo C1-4, haloalquilo C1-4, hidroxialquilo C1-4 e hidroxiaquilo C1-4; L representa un alquileno C1-3; y R7 es cicloalquilo C3-6, fenilo, heterociclo de 4, 5 o 6 miembros y heteroarilo de 5 o 6 miembros, en donde dichos cicloalquilo, fenilo, heterociclo o heteroarilo estan independientemente sin sustituir o sustituidos con 1, 2 o 3 sustituyentes seleccionados independientemente entre halogeno, alquilo C1-3, alcoxi C1-3, en donde dichos alquilo C1-3 y alcoxi C1-3 estan independientemente sin sustituir o sustituidos con 1, 2 o 3 F. Son compuestos preferidos: acido (R)-2-amino-3-[[7-tieno[3,2-b]piridin-2-carbonil]amino]propanoico; acido (R)-2-amino-3-[(7-etiltieno[3,2-b]piridin-2-carbonil)amino]propanoico; acido (R)-2-amino-3-[[7-(difluorometil)tieno[3,2-b]piridin-2-carbonil]amino]propanoico; acido (R)-2-amino-3-[(7-ciclopropiltieno[3,2-b]piridin-2-carbonil)amino]propanoico; entre otros. Dichos compuestos son moduladores del receptor de NMDA y son utiles para tratar trastornos neurologicos o trastornos neuropsiquiatricos tales como la depresion.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201900821 | 2019-07-03 | ||
| PCT/EP2020/068522 WO2021001423A1 (en) | 2019-07-03 | 2020-07-01 | Modulators of the nmda receptor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220137A1 true PE20220137A1 (es) | 2022-01-27 |
Family
ID=74065626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021002225A PE20220137A1 (es) | 2019-07-03 | 2020-07-01 | Moduladores del receptor de nmda |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US11466027B2 (es) |
| EP (1) | EP3994141A1 (es) |
| JP (1) | JP2022539197A (es) |
| KR (1) | KR20220029568A (es) |
| CN (1) | CN114008054A (es) |
| AR (1) | AR119340A1 (es) |
| AU (1) | AU2020299992A1 (es) |
| BR (1) | BR112021003928A2 (es) |
| CA (1) | CA3144304A1 (es) |
| CL (1) | CL2021003557A1 (es) |
| CO (1) | CO2021017142A2 (es) |
| CR (1) | CR20210662A (es) |
| EC (1) | ECSP22003596A (es) |
| IL (1) | IL289575A (es) |
| JO (1) | JOP20210331A1 (es) |
| MA (1) | MA56451A (es) |
| MX (1) | MX2021015742A (es) |
| PE (1) | PE20220137A1 (es) |
| PH (1) | PH12021553286A1 (es) |
| TW (1) | TW202116779A (es) |
| WO (1) | WO2021001423A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021000297A1 (en) | 2019-07-03 | 2021-01-07 | Merck Sharp & Dohme Corp. | Compounds and methods of use thereof as antibacterial agents |
| US11358971B2 (en) | 2019-07-03 | 2022-06-14 | H. Lundbeck A/S | Prodrugs of modulators of the NMDA receptor |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5026700A (en) | 1989-05-16 | 1991-06-25 | Merrell Dow Pharmaceuticals | Certain quinolines and thienopyridines as excitatory amino acid antagonists |
| US5252581A (en) | 1992-07-20 | 1993-10-12 | Hoechst-Roussel Pharmaceuticals Inc. | Substituted aminothienopyridines, pharmaceutical composition and use |
| US6071970A (en) | 1993-02-08 | 2000-06-06 | Nps Pharmaceuticals, Inc. | Compounds active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases |
| KR100366745B1 (ko) | 1994-02-08 | 2003-04-18 | 엔피에스 파마슈티칼즈, 인코포레이티드 | 신경 질환 및 신경 질병의 치료에 유용한 수용체-작동된 칼슘채널의 신규 부위에서 활성인 화합물 |
| JP2002511835A (ja) | 1996-06-07 | 2002-04-16 | エヌピーエス・ファーマシウティカルズ・インコーポレイテッド | 神経障害および神経病の治療に有用な受容体作動性カルシウムチャネル上の新規部位で活性な化合物 |
| WO1998056752A1 (en) | 1997-06-11 | 1998-12-17 | Nps Pharmaceuticals, Inc. | Compounds active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases |
| CL2003002287A1 (es) | 2002-11-25 | 2005-01-14 | Wyeth Corp | COMPUESTOS DERIVADOS DE TIENO[3,2-b]-PIRIDINA-6-CARBONITRILOS Y TIENEO[2,3-b]-PIRIDINA-5-CARBONITRILOS, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION Y COMPUESTOS INTERMEDIARIOS, Y SU USO EN EL TRATAMIENTO DEL CANCER, APOPLEJIA, OSTEOPOROSIS |
| GB0401332D0 (en) | 2004-01-21 | 2004-02-25 | Novartis Ag | Organic compounds |
| GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| US9340555B2 (en) | 2009-09-03 | 2016-05-17 | Allergan, Inc. | Compounds as tyrosine kinase modulators |
| JP5860417B2 (ja) * | 2010-03-04 | 2016-02-16 | メルク・シャープ・エンド・ドーム・コーポレイション | カテコールo−メチルトランスフェラーゼの阻害剤および精神障害の治療におけるその使用 |
| US11358971B2 (en) | 2019-07-03 | 2022-06-14 | H. Lundbeck A/S | Prodrugs of modulators of the NMDA receptor |
-
2020
- 2020-06-30 US US16/916,769 patent/US11466027B2/en active Active
- 2020-07-01 BR BR112021003928-7A patent/BR112021003928A2/pt not_active Application Discontinuation
- 2020-07-01 MX MX2021015742A patent/MX2021015742A/es unknown
- 2020-07-01 AU AU2020299992A patent/AU2020299992A1/en not_active Abandoned
- 2020-07-01 JP JP2021577855A patent/JP2022539197A/ja active Pending
- 2020-07-01 CA CA3144304A patent/CA3144304A1/en active Pending
- 2020-07-01 WO PCT/EP2020/068522 patent/WO2021001423A1/en not_active Ceased
- 2020-07-01 CN CN202080045423.9A patent/CN114008054A/zh active Pending
- 2020-07-01 PE PE2021002225A patent/PE20220137A1/es unknown
- 2020-07-01 MA MA056451A patent/MA56451A/fr unknown
- 2020-07-01 CR CR20210662A patent/CR20210662A/es unknown
- 2020-07-01 PH PH1/2021/553286A patent/PH12021553286A1/en unknown
- 2020-07-01 TW TW109122237A patent/TW202116779A/zh unknown
- 2020-07-01 EP EP20740250.4A patent/EP3994141A1/en not_active Withdrawn
- 2020-07-01 KR KR1020217041215A patent/KR20220029568A/ko not_active Withdrawn
- 2020-07-02 AR ARP200101878A patent/AR119340A1/es not_active Application Discontinuation
-
2021
- 2021-12-14 JO JOP/2021/0331A patent/JOP20210331A1/ar unknown
- 2021-12-15 CO CONC2021/0017142A patent/CO2021017142A2/es unknown
- 2021-12-29 CL CL2021003557A patent/CL2021003557A1/es unknown
-
2022
- 2022-01-02 IL IL289575A patent/IL289575A/en unknown
- 2022-01-17 EC ECSENADI20223596A patent/ECSP22003596A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MA56451A (fr) | 2022-05-11 |
| CL2021003557A1 (es) | 2022-08-19 |
| CA3144304A1 (en) | 2021-01-07 |
| TW202116779A (zh) | 2021-05-01 |
| ECSP22003596A (es) | 2022-02-25 |
| JOP20210331A1 (ar) | 2021-12-14 |
| AR119340A1 (es) | 2021-12-09 |
| AU2020299992A1 (en) | 2022-02-24 |
| CN114008054A (zh) | 2022-02-01 |
| BR112021003928A2 (pt) | 2021-05-18 |
| PH12021553286A1 (en) | 2022-08-01 |
| CR20210662A (es) | 2022-03-02 |
| US11466027B2 (en) | 2022-10-11 |
| JP2022539197A (ja) | 2022-09-07 |
| IL289575A (en) | 2022-03-01 |
| CO2021017142A2 (es) | 2022-01-17 |
| KR20220029568A (ko) | 2022-03-08 |
| WO2021001423A1 (en) | 2021-01-07 |
| US20210002292A1 (en) | 2021-01-07 |
| MX2021015742A (es) | 2022-01-27 |
| EP3994141A1 (en) | 2022-05-11 |
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