AR078958A1 - Derivados de oxazolina, su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por los receptores taar1 - Google Patents
Derivados de oxazolina, su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por los receptores taar1Info
- Publication number
- AR078958A1 AR078958A1 ARP100104164A ARP100104164A AR078958A1 AR 078958 A1 AR078958 A1 AR 078958A1 AR P100104164 A ARP100104164 A AR P100104164A AR P100104164 A ARP100104164 A AR P100104164A AR 078958 A1 AR078958 A1 AR 078958A1
- Authority
- AR
- Argentina
- Prior art keywords
- halogen
- lower alkyl
- substituted
- optionally substituted
- disorders
- Prior art date
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 4
- 101000890887 Homo sapiens Trace amine-associated receptor 1 Proteins 0.000 title abstract 2
- 102100040114 Trace amine-associated receptor 1 Human genes 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 150000002918 oxazolines Chemical class 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 24
- 150000002367 halogens Chemical group 0.000 abstract 24
- 125000000217 alkyl group Chemical group 0.000 abstract 21
- 125000003545 alkoxy group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 208000035475 disorder Diseases 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 abstract 1
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000017164 Chronobiology disease Diseases 0.000 abstract 1
- 208000020401 Depressive disease Diseases 0.000 abstract 1
- 208000002249 Diabetes Complications Diseases 0.000 abstract 1
- 206010012655 Diabetic complications Diseases 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- 208000030814 Eating disease Diseases 0.000 abstract 1
- 208000019454 Feeding and Eating disease Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 1
- 208000019695 Migraine disease Diseases 0.000 abstract 1
- XCUAIINAJCDIPM-XVFCMESISA-N N(4)-hydroxycytidine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=NO)C=C1 XCUAIINAJCDIPM-XVFCMESISA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 230000036760 body temperature Effects 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 230000027288 circadian rhythm Effects 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 235000014632 disordered eating Nutrition 0.000 abstract 1
- 238000005265 energy consumption Methods 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 230000013632 homeostatic process Effects 0.000 abstract 1
- 230000007257 malfunction Effects 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 206010027599 migraine Diseases 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 201000009032 substance abuse Diseases 0.000 abstract 1
- 231100000736 substance abuse Toxicity 0.000 abstract 1
- 208000011117 substance-related disease Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/28—Nitrogen atoms not forming part of a nitro radical
-
- 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
- A61K31/42—Oxazoles
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
-
- 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
- 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
- A61P25/06—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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/20—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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- 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
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- C07D403/10—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
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
- C07D413/02—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
-
- 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
-
- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Nutrition Science (AREA)
- Addiction (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
Abstract
Se ha constatado que los compuestos de la formula 1 tienen afinidad con los receptores asociados con las aminas traza (TAARs), en especial con el TAAR1. Los compuestos pueden utilizarse para el tratamiento de la depresion, los trastornos de ansiedad, el trastorno bipolar, el trastorno de hiperactividad con déficit de atencion (ADHD), los trastornos relacionados con el estrés, los trastornos psicoticos como la esquizofrenia, las enfermedades neurologicas como la enfermedad de Parkinson, los trastornos neurodegenerativos, por ejemplo la enfermedad de Alzheimer, la epilepsia, la migrana, la hipertension, el abuso de sustancias y los trastornos metabolicos como son los trastornos de ingestion de comida, la diabetes, las complicaciones diabéticas, la obesidad, la dislipidemia, los trastornos de consumo y asimilacion de energía, los trastornos y malfuncion de la temperatura corporal, la homeostasis, los trastornos del sueno y del ritmo circadiano y los trastornos cardiovasculares. Reivindicacion 1: Compuestos de la formula (1) en la que Ra es hidrogeno o alquilo inferior; R1 es grupo (2) o puede elegirse entre el grupo formado por (3); R8 es hidrogeno, halogeno o arilo opcionalmente sustituido por halogeno; X es un enlace, -(CH2)n-, -CHRCH2, -CHR(CH2)2-, -O-CHRCH2- o (4); y R es alquilo inferior o alquilo inferior sustituido por halogeno; R2 es a) alquilo inferior; b) hidrogeno; c) NR-arilo, opcionalmente sustituido por uno o más sustituyentes elegidos entre halogeno y alquilo inferior sustituido por halogeno; d) NH-heteroarilo, opcionalmente sustituido por uno o más sustituyentes elegidos entre halogeno y alquilo inferior sustituido por halogeno; e) (CR'R'')m-cicloalquilo opcionalmente sustituido por halogeno, alquilo inferior, alquilo inferior sustituido por halogeno, fenilo sustituido por halogeno o por heteroarilo; f) heterocicloalquilo opcionalmente sustituido por halogeno o alquilo inferior sustituido por halogeno; g) (CR'R'')m-heteroarilo opcionalmente sustituido por halogeno, alcoxi inferior, alquilo inferior sustituido por halogeno, alcoxi inferior sustituido por halogeno, alquilo inferior, cicloalquilo, NHC(O)-alquilo inferior, ciano, S(O)2-alquilo inferior, NR6R7, o por heteroarilo o por heterociclilo que está opcionalmente sustituido por halogeno; h) (CR'R'')m-arilo opcionalmente sustituido por halogeno, alquilo inferior sustituido por halogeno, alcoxi inferior sustituido por halogeno, alquilo inferior, alquinilo, alcoxi inferior, CH2-alcoxi inferior o ciano; i) -O(CH2)o-arilo opcionalmente sustituido por halogeno, alcoxi inferior o alquilo inferior sustituido por halogeno; R' y R'' con independencia entre sí son hidrogeno, alcoxi inferior o alquilo inferior; o junto con el átomo de C pueden formar un grupo cicloalquilo; R3 es arilo o heteroarilo, cuyos anillos aromáticos están opcionalmente sustituidos por uno o más sustituyentes elegidos entre halogeno y alcoxi inferior; R4 es alquilo inferior, arilo o heteroarilo, cuyos anillos aromáticos están opcionalmente sustituidos por uno o más sustituyentes elegidos entre halogeno, ciano y alcoxi inferior; R5 es hidrogeno, alquilo inferior o arilo sustituido por halogeno; o R4 y R5 junto con el átomo de N al que están unidos pueden formar un anillo heterocíclico; R6/R7 con independencia entre sí son hidrogeno, alquilo inferior o (CH2)2-O-alquilo inferior; m es el numero 0, 1 o 2; n es el numero 1, 2 o 3; o es el numero 0 o 1; p es el numero 0, 1 o 2; o una sal de adicion de ácido farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09175712 | 2009-11-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078958A1 true AR078958A1 (es) | 2011-12-14 |
Family
ID=43506400
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104164A AR078958A1 (es) | 2009-11-11 | 2010-11-10 | Derivados de oxazolina, su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por los receptores taar1 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8354441B2 (es) |
| EP (1) | EP2499121B1 (es) |
| JP (1) | JP5552539B2 (es) |
| KR (1) | KR101461294B1 (es) |
| CN (1) | CN102686572A (es) |
| AR (1) | AR078958A1 (es) |
| BR (1) | BR112012011105A2 (es) |
| CA (1) | CA2780568A1 (es) |
| ES (1) | ES2550976T3 (es) |
| MX (1) | MX2012005363A (es) |
| RU (1) | RU2569887C2 (es) |
| TW (1) | TW201121543A (es) |
| WO (1) | WO2011057973A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2305672B1 (en) | 2008-06-13 | 2019-03-27 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
| US9132136B2 (en) * | 2010-08-02 | 2015-09-15 | Hoffmann-La Roche Inc. | Pharmaceutical combination |
| US8673950B2 (en) * | 2010-11-02 | 2014-03-18 | Hoffmann-Laroche Inc. | Dihydrooxazol-2-amine derivatives |
| US9073911B2 (en) | 2011-06-09 | 2015-07-07 | Hoffmann-La Roche Inc. | Pyrazole derivatives |
| US9029370B2 (en) | 2011-06-10 | 2015-05-12 | Hoffmann-La Roche Inc. | Substituted benzamide derivatives |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| CN105272975B (zh) * | 2014-06-10 | 2019-03-26 | 中国科学院上海药物研究所 | 一类具有1,2,4-恶二唑片段结构的吲哚生物碱及其制备方法和用途 |
| WO2017210616A1 (en) * | 2016-06-02 | 2017-12-07 | Purdue Pharma L.P. | Trace amine associated receptor 1 agonists and partial agonists for pain treatment |
| AU2022309257A1 (en) * | 2021-07-12 | 2024-01-04 | Fortephest Ltd | Novel derivatives of non-coded amino acids and their use as herbicides |
| EP4638433A1 (en) * | 2022-12-22 | 2025-10-29 | Cytokinetics, Inc. | Nampt modulators |
| CN116496496B (zh) * | 2023-04-27 | 2024-11-05 | 中国石油大学(华东) | 一种基于三嗪共价框架材料(CTFs)制备单位点催化剂的制备方法 |
Family Cites Families (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2731471A (en) | 1956-01-17 | Nxg hi | ||
| US2161938A (en) | 1934-07-31 | 1939-06-13 | Soc Of Chemical Ind | Imidazolines |
| US2457047A (en) | 1946-02-13 | 1948-12-21 | Monsanto Chemicals | 2-(2'-thenyl)-4, 5-dihydroimidazoles and process for making the same |
| DE842065C (de) | 1950-07-30 | 1952-06-23 | Bayer Ag | Verfahren zur Herstellung stickstoffhaltiger heterocyclischer Verbindungen |
| US2778836A (en) | 1954-04-02 | 1957-01-22 | Union Chimique Belge Sa | Substituted 2-methyl-delta2 imidazolines |
| US2744910A (en) | 1955-06-27 | 1956-05-08 | Bristol Lab Inc | 2-(ortho-benzylbenzyl)-imidazoline and acid addition salts |
| US2744909A (en) | 1955-06-27 | 1956-05-08 | Bristol Lab Inc | 2-(ortho-phenylbenzyl) imidazoline and acid addition salts |
| US2919274A (en) | 1957-09-17 | 1959-12-29 | Sahyun Melville | Amidines |
| GB877306A (en) | 1958-04-21 | 1961-09-13 | Pfizer & Co C | Halogenated derivatives of tetrahydro-1-naphthyl cyclic amidines |
| DE1121054B (de) | 1960-11-23 | 1962-01-04 | Merck Ag E | Verfahren zur Herstellung eines neuen Imidazolinderivates und dessen Saeureadditionssalzen |
| US3190802A (en) | 1961-10-09 | 1965-06-22 | Boehringer Sohn Ingelheim | Shaving composition and method of using same |
| FR1355049A (fr) | 1962-04-12 | 1964-03-13 | Merck Ag E | Agent pour le traitement préalable de la peau en vue du rasage |
| DE1150180B (de) | 1962-04-12 | 1963-06-12 | Merck Ag E | Mittel zur Vorbehandlung der Haut fuer die Rasur |
| ES323985A1 (es) | 1966-02-26 | 1966-12-16 | Blade Pique Juan | Procedimiento para la obtenciën de derivados del imidazol |
| US3377247A (en) | 1967-04-28 | 1968-04-09 | Dow Chemical Co | Antidepressant method |
| US3586695A (en) | 1968-01-26 | 1971-06-22 | Dow Chemical Co | Substituted imidazolinyl indoles |
| US3577428A (en) | 1969-04-14 | 1971-05-04 | Colgate Palmolive Co | 2-amino-4-aryloxyalkyl-4-alkyl-2-oxazolines |
| BE754935A (fr) | 1969-08-13 | 1971-02-17 | Hoechst Ag | 2-(thienyl-3'-amino)-1,3-diazacycloalcenes et leur preparation |
| US3818094A (en) | 1969-08-28 | 1974-06-18 | Boehringer Sohn Ingelheim | Hypotensive pharmaceutical compositions containing certain 2-anilino-1,3-diazacyclopentenes-(2) |
| US3622579A (en) | 1969-08-28 | 1971-11-23 | Boehringer Sohn Ingelheim | Derivatives of 2-anilino-1,3-diazacyclopentene-(2) |
| US3660423A (en) | 1970-02-13 | 1972-05-02 | Dow Chemical Co | 2-(substituted benzyl)methyl-2-imidazolines |
| GB1333471A (en) | 1971-01-27 | 1973-10-10 | Labaz | Imidazoline derivatives and process for preparing the same |
| HU167760B (es) * | 1972-10-20 | 1975-12-25 | ||
| DE2253555A1 (de) | 1972-11-02 | 1974-05-09 | Hoechst Ag | Oxazolo-pyrimidine und verfahren zu ihrer herstellung |
| DE2446758C3 (de) | 1974-10-01 | 1979-01-04 | C.H. Boehringer Sohn, 6507 Ingelheim | 2-(2-Fluor-6-trifluormethylphenylimino)-imidazolidin, dessen Säureadditionssalze, Verfahren zur Herstellung dieser Verbindungen und deren Verwendung bei der Bekämpfung der Hypertonie |
| US4125620A (en) | 1974-10-01 | 1978-11-14 | Boehringer Ingelheim Gmbh | 2-[(2',6'-Disubstituted-phenyl)-imino]-imidazolidines and salts thereof |
| US3992403A (en) | 1975-05-30 | 1976-11-16 | Schering Corporation | 2-Imidazolines and their use as hypoglycemic agents |
| GB1538097A (en) | 1976-01-26 | 1979-01-10 | Lafon Labor | Substituted phenyl-amidines |
| DE2849537C2 (de) | 1978-11-15 | 1983-03-17 | Beiersdorf Ag, 2000 Hamburg | Substituierte 5-(2-Imidazolin-2-yl)-aminopyrimidine, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel |
| US4323570A (en) | 1978-11-15 | 1982-04-06 | Beiersdorf Aktiengesellschaft | Substituted aminopyrimidines |
| AU518569B2 (en) | 1979-08-07 | 1981-10-08 | Farmos-Yhtyma Oy | 4-benzyl- and 4-benzoyl imidazole derivatives |
| US4311840A (en) | 1980-11-13 | 1982-01-19 | E. R. Squibb & Sons, Inc. | 2,3,6,7-Tetrahydro-2-thioxo-4H-oxazolo[3,2-a]-1,3,5 triazin-4-ones |
| US4540705A (en) | 1983-03-14 | 1985-09-10 | Sterling Drug Inc. | Antidepressant imidazolines and related compounds |
| DE3316554C1 (de) | 1983-05-06 | 1984-07-12 | Dr. Johannes Heidenhain Gmbh, 8225 Traunreut | Verdampfervorrichtung mit Strahlheizung zum Aufdampfen mehrerer Materialien |
| DE3583900D1 (de) | 1984-06-06 | 1991-10-02 | Abbott Lab | Adrenergische verbindungen. |
| DK302185A (da) | 1984-07-05 | 1986-01-06 | Rolland Sa A | 2-amino-oxazoliner samt fremgangsmaade til deres fremstilling |
| US4665095A (en) | 1985-12-11 | 1987-05-12 | Abbott Laboratories | Use of 2-[(3,5-dihalo-4-aminobenzyl)]imidazolines to stimulate alpha-1 adrenergic receptors and to treat nasal congestion |
| GB2215206B (en) | 1988-02-29 | 1991-07-03 | Farmos Oy | 4-substituted imidazole derivatives useful in perioperative care |
| FR2645860B1 (fr) | 1989-04-14 | 1991-07-26 | Sarget Lab | Nouvelles aryloxymethyl-5 amino-2 oxazolines, syntheses et applications therapeutiques |
| FI894911A0 (fi) | 1989-10-17 | 1989-10-17 | Farmos Oy | En terapeutiskt vaerdefull foerening. |
| CA2211325C (en) | 1993-10-13 | 2006-08-15 | H. Joseph Horacek | Extended release clonidine formulation |
| GB9425211D0 (en) | 1994-12-14 | 1995-02-15 | Ucb Sa | Substituted 1H-imidazoles |
| DE19514579A1 (de) | 1995-04-20 | 1996-10-24 | Boehringer Ingelheim Kg | Verwendung von alpha¶1¶¶L¶-Agonisten zur Behandlung der Harninkontinenz |
| US5610174A (en) | 1995-06-02 | 1997-03-11 | Synaptic Pharmaceutical Corporation | Use of α1A -selective adrenoceptor agonists for the treatment of urinary incontinence |
| GB9520150D0 (en) | 1995-10-03 | 1995-12-06 | Orion Yhtymae Oy | New imidazole derivatives |
| US5969137A (en) | 1996-09-19 | 1999-10-19 | Virginia Commonwealth University | Benzylamidine derivatives with serotonin receptor binding activity |
| ZA981029B (en) | 1997-02-11 | 1999-08-10 | Lilly Co Eli | Pharmaceutical agents. |
| US5866579A (en) | 1997-04-11 | 1999-02-02 | Synaptic Pharmaceutical Corporation | Imidazole and imidazoline derivatives and uses thereof |
| US6841684B2 (en) | 1997-12-04 | 2005-01-11 | Allergan, Inc. | Imidiazoles having reduced side effects |
| PL341009A1 (en) | 1997-12-04 | 2001-03-12 | Allergan Sales | Substitute derivatives of imidazole exhibiting agonist-like activity in respect to adrenergic alpha 2b or 2b/2c receptors |
| CA2315226A1 (en) | 1997-12-19 | 1999-07-01 | Eli Lilly And Company | Hypoglycemic imidazoline compounds |
| CA2328973A1 (en) | 1998-04-23 | 1999-10-28 | Akio Ojida | Naphthalene derivatives, their production and use |
| ES2150378B1 (es) | 1998-08-07 | 2001-07-01 | Esteve Labor Dr | Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p. |
| CA2246027A1 (en) | 1998-08-27 | 2000-02-27 | Virginia Commonwealth University | Benzylamidine derivatives with serotonin receptor binding activity |
| PE20010781A1 (es) | 1999-10-22 | 2001-08-08 | Takeda Chemical Industries Ltd | Compuestos 1-(1h-imidazol-4-il)-1-(naftil-2-sustituido)etanol, su produccion y utilizacion |
| JP2001302643A (ja) | 2000-04-21 | 2001-10-31 | Suntory Ltd | 環状アミジン化合物 |
| CA2422288A1 (en) | 2000-09-12 | 2002-03-21 | Oregon Health & Science University | Novel mammalian receptor genes and uses |
| EP1339694B1 (en) | 2000-11-14 | 2005-09-21 | F. Hoffmann-La Roche Ag | Substituted 2-phenylaminoimidazoline phenyl ketone derivatives as ip antagonists |
| IL147921A0 (en) | 2002-01-31 | 2002-08-14 | Abdulrazik Mohammad | A method for treating central nervous system disorders by ocular dosing |
| TW200930291A (en) | 2002-04-29 | 2009-07-16 | Bayer Cropscience Ag | Pesticidal heterocycles |
| KR100492252B1 (ko) | 2002-08-09 | 2005-05-30 | 한국화학연구원 | 이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법 |
| US20090209422A1 (en) | 2005-05-03 | 2009-08-20 | Bayer Cropscience Ag | Insecticidal Substituted Aminoalkyl Heterocyclic and Heteroaryl Derivatives |
| BRPI0615307A2 (pt) | 2005-08-25 | 2009-08-04 | Schering Corp | agonistas de adrenorreceptor alfa2c |
| AU2007209381A1 (en) * | 2006-01-27 | 2007-08-02 | F. Hoffmann-La Roche Ag | Use of substituted 2-imidazole of imidazoline derivatives |
| KR101079914B1 (ko) | 2006-01-27 | 2011-11-04 | 에프. 호프만-라 로슈 아게 | 중추신경계 장애를 위한 4-이미다졸 유도체의 용도 |
| WO2007088155A1 (de) * | 2006-01-31 | 2007-08-09 | Corpac Deutschland Gmbh & Co. Kg | Haube oder deckel, insbesondere für behälter für korrosionsempfindliche ladung |
| US7691863B2 (en) | 2006-10-04 | 2010-04-06 | Hoffman-La Roche Inc. | Pyrazine-2-carboxamide derivatives as CB2 receptor modulators |
| CA2666762C (en) * | 2006-10-19 | 2014-12-30 | F. Hoffmann-La Roche Ag | Aminomethyl-4-imidazoles |
| WO2008092785A1 (en) | 2007-02-02 | 2008-08-07 | F. Hoffmann-La Roche Ag | Novel 2-aminooxazolines as taar1 ligands for cns disorders |
| KR101222412B1 (ko) | 2007-02-15 | 2013-01-15 | 에프. 호프만-라 로슈 아게 | Taar1 리간드로서의 2-아미노옥사졸린 |
| CN101952260B (zh) | 2008-02-18 | 2013-02-13 | 弗·哈夫曼-拉罗切有限公司 | 4,5-二氢-*唑-2-基胺衍生物 |
| CN102083805A (zh) | 2008-07-24 | 2011-06-01 | 弗·哈夫曼-拉罗切有限公司 | 4,5-二氢-唑-2-基衍生物 |
| TW201026672A (en) | 2008-10-07 | 2010-07-16 | Schering Corp | Spiroaminooxazoline analogues as alpha2C adrenergic receptor modulators |
-
2010
- 2010-11-03 US US12/938,401 patent/US8354441B2/en not_active Expired - Fee Related
- 2010-11-08 ES ES10779293.9T patent/ES2550976T3/es active Active
- 2010-11-08 EP EP10779293.9A patent/EP2499121B1/en not_active Not-in-force
- 2010-11-08 CN CN2010800512387A patent/CN102686572A/zh active Pending
- 2010-11-08 KR KR1020127014785A patent/KR101461294B1/ko not_active Expired - Fee Related
- 2010-11-08 TW TW099138394A patent/TW201121543A/zh unknown
- 2010-11-08 CA CA2780568A patent/CA2780568A1/en not_active Abandoned
- 2010-11-08 RU RU2012121684/04A patent/RU2569887C2/ru not_active IP Right Cessation
- 2010-11-08 WO PCT/EP2010/066960 patent/WO2011057973A1/en not_active Ceased
- 2010-11-08 MX MX2012005363A patent/MX2012005363A/es active IP Right Grant
- 2010-11-08 JP JP2012538290A patent/JP5552539B2/ja not_active Expired - Fee Related
- 2010-11-08 BR BR112012011105A patent/BR112012011105A2/pt not_active IP Right Cessation
- 2010-11-10 AR ARP100104164A patent/AR078958A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2780568A1 (en) | 2011-05-19 |
| CN102686572A (zh) | 2012-09-19 |
| JP2013510812A (ja) | 2013-03-28 |
| WO2011057973A1 (en) | 2011-05-19 |
| KR101461294B1 (ko) | 2014-11-12 |
| TW201121543A (en) | 2011-07-01 |
| KR20120092655A (ko) | 2012-08-21 |
| MX2012005363A (es) | 2012-05-29 |
| US20110112080A1 (en) | 2011-05-12 |
| EP2499121B1 (en) | 2015-10-07 |
| US8354441B2 (en) | 2013-01-15 |
| BR112012011105A2 (pt) | 2019-09-24 |
| EP2499121A1 (en) | 2012-09-19 |
| ES2550976T3 (es) | 2015-11-13 |
| RU2012121684A (ru) | 2013-12-20 |
| JP5552539B2 (ja) | 2014-07-16 |
| WO2011057973A9 (en) | 2012-02-02 |
| RU2569887C2 (ru) | 2015-12-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR078958A1 (es) | Derivados de oxazolina, su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por los receptores taar1 | |
| AR079542A1 (es) | Derivados de benzamida sustituidos, proceso para su preparacion y su uso en el tratamiento de enfermedades mediadas por taars. | |
| ECSP12012098A (es) | Derivados de arilmetoxi isoindolina y composiciones que los comprenden y métodos para utilizar los mismos | |
| DOP2012000167A (es) | Moduladores alostericos positivos de receptores m1 de la quinolina amida | |
| CO6321133A2 (es) | Nuevas 2-aminooxazolinas como ligandos taar1 para trastornos cns | |
| ECSP13012896A (es) | Derivados heterocíclicos de amina | |
| UA113051C2 (xx) | Гетероциклічні похідні та їх застосування у лікуванні неврологічних розладів | |
| ECSP13013072A (es) | Derivados de pirazol | |
| MX2015003653A (es) | Derivados de amida del acido benzoimidazol-carboxilico como moduladores del receptor apj. | |
| EA201200002A1 (ru) | Производные индоламида и родственные соединения для использования при лечении нейродегенеративных заболеваний | |
| ECSP13013048A (es) | Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores | |
| CL2007003261A1 (es) | Compuestos derivados de 1,4-benzotiepina-1,1-dioxido; composicion farmaceutica; y su uso para el tratamiento de trastornos del metabolismo de lipidos, hiperlipidemia, resistencia a la insulina, diabetes y trastornos del snc, tales como esquizofrenia, | |
| BR112014023384A8 (pt) | inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos. | |
| MX2010009658A (es) | Derivados de azetidina. | |
| EA201170705A1 (ru) | Арилметилбензохиназолиноны в качестве позитивных аллостерических модуляторов рецептора м1 | |
| ECSP11010782A (es) | Derivados de 4,5-dihidro-oxazol-2-ilo | |
| CL2013003485A1 (es) | Compuestos derivados de benzamida sustituida como moduladores de receptores asociados con las aminas traza (taar1); composición farmacéutica; procedimiento de preparación; y uso en el tratamiento de depresión, psicosis, enfermedad de parkinson, ansiedad, trastorno de hiperactividad (adhd) y diabetes. | |
| ATE525350T1 (de) | Substituierte n-phenyl- bipyrrolidincarbonsäureamide und deren therapeutische verwendung | |
| AR089691A1 (es) | Derivados heterociclicos | |
| ECSP11010947A (es) | Compuestos n- sulfonamido pirazolil policíclicos | |
| TW200833697A (en) | Spiro-piperidine derivatives | |
| PE20150735A1 (es) | Derivados de pirazol-carboxamida como moduladores de taar para uso en el tratamiento de numerosos desordenes, tales como depresion, diabetes y enfermedad de parkinson | |
| MX377195B (es) | Derivados de morfolina-piridina. | |
| AR076979A1 (es) | 2- aminooxazolinas como ligandos de taar1 | |
| TW200833696A (en) | Spiro-piperidine derivatives |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |