MX2016008842A - Derivados de n-fenil-lactama capaces de estimular la neurogenesis y su uso en el tratamiento de trastornos neurologicos. - Google Patents
Derivados de n-fenil-lactama capaces de estimular la neurogenesis y su uso en el tratamiento de trastornos neurologicos.Info
- Publication number
- MX2016008842A MX2016008842A MX2016008842A MX2016008842A MX2016008842A MX 2016008842 A MX2016008842 A MX 2016008842A MX 2016008842 A MX2016008842 A MX 2016008842A MX 2016008842 A MX2016008842 A MX 2016008842A MX 2016008842 A MX2016008842 A MX 2016008842A
- Authority
- MX
- Mexico
- Prior art keywords
- halogen
- lower alkyl
- phenyl
- lower alkoxy
- substituted
- Prior art date
Links
- 208000012902 Nervous system disease Diseases 0.000 title 1
- 208000025966 Neurological disease Diseases 0.000 title 1
- 230000004766 neurogenesis Effects 0.000 title 1
- 230000004936 stimulating effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical class 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- -1 oxazole-5-yl Chemical group 0.000 abstract 3
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 102000014461 Ataxins Human genes 0.000 abstract 1
- 108010078286 Ataxins Proteins 0.000 abstract 1
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 206010008025 Cerebellar ataxia Diseases 0.000 abstract 1
- 208000027104 Chemotherapy-Related Cognitive Impairment Diseases 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 206010011878 Deafness Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 201000007737 Retinal degeneration Diseases 0.000 abstract 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 208000009205 Tinnitus Diseases 0.000 abstract 1
- 208000030886 Traumatic Brain injury Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000032683 aging Effects 0.000 abstract 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 1
- 208000029560 autism spectrum disease Diseases 0.000 abstract 1
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 abstract 1
- 230000037326 chronic stress Effects 0.000 abstract 1
- 229960003920 cocaine Drugs 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 230000010370 hearing loss Effects 0.000 abstract 1
- 231100000888 hearing loss Toxicity 0.000 abstract 1
- 208000016354 hearing loss disease Diseases 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 229960001252 methamphetamine Drugs 0.000 abstract 1
- MYWUZJCMWCOHBA-VIFPVBQESA-N methamphetamine Chemical compound CN[C@@H](C)CC1=CC=CC=C1 MYWUZJCMWCOHBA-VIFPVBQESA-N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 208000030459 obsessive-compulsive personality disease Diseases 0.000 abstract 1
- 229940127240 opiate Drugs 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 208000019906 panic disease Diseases 0.000 abstract 1
- JTJMJGYZQZDUJJ-UHFFFAOYSA-N phencyclidine Chemical compound C1CCCCN1C1(C=2C=CC=CC=2)CCCCC1 JTJMJGYZQZDUJJ-UHFFFAOYSA-N 0.000 abstract 1
- 229950010883 phencyclidine Drugs 0.000 abstract 1
- 208000028173 post-traumatic stress disease Diseases 0.000 abstract 1
- 238000001959 radiotherapy Methods 0.000 abstract 1
- 230000004258 retinal degeneration Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 208000020431 spinal cord injury Diseases 0.000 abstract 1
- 231100000886 tinnitus Toxicity 0.000 abstract 1
- 230000009529 traumatic brain injury Effects 0.000 abstract 1
Classifications
-
- 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
- C07D403/10—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 carbon chain containing aromatic 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
- C07D413/10—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 carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
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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
- C07D401/10—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 aromatic rings
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la fórmula general I en donde Het es oxazol-5-ilo, piridin-4-ilo, o pirazol-4-ilo; R1/R2 son, independientemente uno de otro, hidrógeno, alquilo inferior, alcoxi inferior, o halógeno; W es -CH2- o -CH2CH2-; X es CR3R4 o NR5 R3 es hidrógeno o alquilo inferior; R4 es -(CH2)n-fenilo, opcionalmente sustituido por halógeno, alcoxi inferior, alquilo inferior sustituido por halógeno, alcoxi inferior sustituido por halógeno o alquilo inferior; R5 es CHR-fenilo o CH2CHR-fenilo, opcionalmente sustituido por halógeno, alcoxi inferior, alquilo inferior sustituido por halógeno, alcoxi inferior sustituido por halógeno o alquilo inferior, o es CHR-piridin-2, 3 o 4-ilo; R es hidrógeno o alquilo inferior; n es 0 o 1; o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica o a su correspondiente enantiómero y/o isómero óptico del mismo. Los compuestos se pueden usar para el tratamiento de la esquizofrenia, trastorno obsesivo-compulsivo de la personalidad, depresión, trastornos bipolares, trastornos de ansiedad, envejecimiento, epilepsia, degeneración de la retina, lesión cerebral traumática, lesión de la médula vertebral normal, trastorno de estrés post-traumático, trastorno de pánico, enfermedad, demencia, enfermedad de Alzheimer, deterioro cognitivo, disfunción cognitiva inducida por quimioterapia, síndrome de Down, trastornos del espectro autista, pérdida, tinnitus, ataxia espinocerebelosa, esclerosis lateral amiotráfica, esclerosis múltiple de la audición, enfermedad, accidente cerebrovascular, la terapia de radiación, el estrés cránico de Huntington de Parkinson, abuso de drogas neuro-activos, seleccionados a partir de alcohol, opiáceos, metanfetamina, fenciclidina y cocaína.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14151754 | 2014-01-20 | ||
| PCT/EP2015/050521 WO2015107053A1 (en) | 2014-01-20 | 2015-01-14 | N-phenyl-lactam derivatives capable of stimulating neurogenesis and their use in the treatment of neurological disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2016008842A true MX2016008842A (es) | 2016-11-08 |
Family
ID=49949591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016008842A MX2016008842A (es) | 2014-01-20 | 2015-01-14 | Derivados de n-fenil-lactama capaces de estimular la neurogenesis y su uso en el tratamiento de trastornos neurologicos. |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9714239B2 (es) |
| EP (1) | EP3097090B1 (es) |
| JP (1) | JP6321825B2 (es) |
| KR (1) | KR101861942B1 (es) |
| CN (1) | CN106061964B (es) |
| CA (1) | CA2935270A1 (es) |
| MX (1) | MX2016008842A (es) |
| RU (1) | RU2016131875A (es) |
| WO (1) | WO2015107053A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2961746B1 (en) | 2013-02-28 | 2018-01-03 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| US9902702B2 (en) | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| US10123993B2 (en) | 2015-01-09 | 2018-11-13 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
| ES2730112T3 (es) | 2015-03-09 | 2019-11-08 | Bristol Myers Squibb Co | Lactamas como inhibidores de ROCK |
| TW201722957A (zh) * | 2015-09-15 | 2017-07-01 | 葛蘭素史克智慧財產(第二)有限公司 | 化學化合物 |
| WO2017046739A1 (en) * | 2015-09-15 | 2017-03-23 | Glaxosmithkline Intellectual Property (No.2) Limited | Imidazolidinone derivatives as inhibitors of perk |
| US10562887B2 (en) * | 2016-05-27 | 2020-02-18 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of ROCK |
| HUE061751T2 (hu) | 2018-02-26 | 2023-08-28 | AlzeCure Pharma AB | Triazinszármazékok neurotrofinokhoz kapcsolódó betegségek kezelésére |
| GB201810668D0 (en) | 2018-06-28 | 2018-08-15 | Stiftelsen Alzecure | New compounds |
| EP3870159B1 (en) | 2018-10-26 | 2024-11-13 | University of South Florida | Drug for treating tinnitus |
| CN119219603A (zh) * | 2023-06-28 | 2024-12-31 | 科辉智药(深圳)新药研究中心有限公司 | Sarm1酶活性抑制剂及其用途 |
| CN120424050A (zh) * | 2024-02-05 | 2025-08-05 | 科辉智药(深圳)新药研究中心有限公司 | 作为sarm1酶活性抑制剂的吡啶类化合物及其应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1051765C (zh) * | 1996-06-25 | 2000-04-26 | 厦门大学 | 一种立体选择性合成对映体纯3-氨基-1,2-二取代吡咯烷的方法 |
| AU2005223481A1 (en) * | 2004-03-17 | 2005-09-29 | Pfizer Products Inc. | Novel benzyl(idene)-lactam derivatives |
| WO2007026219A2 (en) * | 2005-08-31 | 2007-03-08 | Pfizer Products Inc. | Combinations of a 5-ht1b antagonist with a noradrenalin re-uptake inhibitor or a serotonin noradrenalin reutake inhibitor for treating cns conditions |
| WO2007026224A2 (en) * | 2005-08-31 | 2007-03-08 | Pfizer Products Inc. | 5-ht1b antagonist composition for depression, anxiety and cognition |
| EP2019093A4 (en) * | 2006-05-19 | 2011-02-23 | Eisai R&D Man Co Ltd | CINEMA ACID AMID DERIVATIVE FROM THE UREA TYPE |
| WO2008046072A2 (en) | 2006-10-13 | 2008-04-17 | The Board Of Regents Of The University Of Texas System | Chemical inducers of neurogenesis |
| WO2008137102A2 (en) * | 2007-05-04 | 2008-11-13 | Torreypines Therapeutics, Inc. | Methods of modulating amyloid beta and compounds useful therefor |
| WO2009078992A1 (en) * | 2007-12-17 | 2009-06-25 | Amgen Inc. | Linear tricyclic compounds as p38 kinase inhibitors |
| US9095572B2 (en) | 2009-01-09 | 2015-08-04 | Board Of Regents Of The University Of Texas System | Pro-neurogenic compounds |
| WO2011007819A1 (ja) * | 2009-07-17 | 2011-01-20 | 塩野義製薬株式会社 | ラクタムまたはベンゼンスルホンアミド化合物を含有する医薬 |
| TWI468402B (zh) * | 2009-07-31 | 2015-01-11 | 必治妥美雅史谷比公司 | 降低β-類澱粉生成之化合物 |
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2015
- 2015-01-14 CN CN201580003762.XA patent/CN106061964B/zh not_active Expired - Fee Related
- 2015-01-14 CA CA2935270A patent/CA2935270A1/en not_active Abandoned
- 2015-01-14 JP JP2016564394A patent/JP6321825B2/ja not_active Expired - Fee Related
- 2015-01-14 KR KR1020167022497A patent/KR101861942B1/ko not_active Expired - Fee Related
- 2015-01-14 EP EP15700244.5A patent/EP3097090B1/en active Active
- 2015-01-14 WO PCT/EP2015/050521 patent/WO2015107053A1/en not_active Ceased
- 2015-01-14 MX MX2016008842A patent/MX2016008842A/es unknown
- 2015-01-14 RU RU2016131875A patent/RU2016131875A/ru not_active Application Discontinuation
-
2016
- 2016-07-19 US US15/213,622 patent/US9714239B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| KR20160108545A (ko) | 2016-09-19 |
| EP3097090A1 (en) | 2016-11-30 |
| RU2016131875A (ru) | 2018-02-26 |
| US20160326150A1 (en) | 2016-11-10 |
| CN106061964A (zh) | 2016-10-26 |
| CA2935270A1 (en) | 2015-07-23 |
| EP3097090B1 (en) | 2018-10-10 |
| JP6321825B2 (ja) | 2018-05-09 |
| JP2017503025A (ja) | 2017-01-26 |
| WO2015107053A1 (en) | 2015-07-23 |
| CN106061964B (zh) | 2019-10-25 |
| KR101861942B1 (ko) | 2018-06-29 |
| RU2016131875A3 (es) | 2018-08-09 |
| US9714239B2 (en) | 2017-07-25 |
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