AR032653A1 - Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos. - Google Patents
Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos.Info
- Publication number
- AR032653A1 AR032653A1 ARP020100370A ARP020100370A AR032653A1 AR 032653 A1 AR032653 A1 AR 032653A1 AR P020100370 A ARP020100370 A AR P020100370A AR P020100370 A ARP020100370 A AR P020100370A AR 032653 A1 AR032653 A1 AR 032653A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- compounds
- aryl
- transporter
- heteroaryl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
- C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the 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
-
- 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
- A61K31/4196—1,2,4-Triazoles
-
- 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
- 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
- A61K31/433—Thidiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/08—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
- A61P25/18—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
-
- 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
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
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)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Provee compuestos, composiciones y métodos para inhibir al transportador de glicina 2 y para afectar la actividad neuronal mediada por el transportador de glicina. Los compuestos utiles comprenden a los compuestos de la formula (1) donde: n es 0, 1, 2 o 3 y R es independientemente, halogeno, hidroxi, alquilo inferior opcionalmente sustituido con halogeno o alcoxi menor opcionalmente sustituido con halogeno; X es O, S o N-R' (donde R' es alquilo inferior, arilo, heteroarilo, arilo-menor alquileno o heteroarilo-menor alquileno); Q puede estar ausente o presente, y cuando está presente, está representado por la formula (2) donde n, R y X son como definimos anteriormente; donde Q está presente, W es un alquileno menor y cuando Q está ausente, W está opcionalmente sustituido con alquilo inferior, opcionalmente sustituido con arilo opcionalmente sustituido con heteroarilo (opcionalmente arilo sustituido)-X-CH2- donde X es como definimos anteriormente; o su sal farmacéuticamente aceptable. Estos compuestos son particularmente utiles para tratar enfermedades nerviosas y musculares, incluyendo a la psicosis, dolor, epilepsia, enfermedades neurodegenerativas, apoplejía, trauma encefálico, esclerosis multiple y similares, y trastornos musculares, incluyendo a las enfermedades o condiciones asociadas con la contraccion aumentada del musculo, como por ejemplo, la espasticidad y mioclonus. Además, se pueden utilizar los compuestos para descubrir otros agentes con una actividad mejorada en los ensayos donde son activos los compuestos de la invencion.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US26789401P | 2001-02-09 | 2001-02-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR032653A1 true AR032653A1 (es) | 2003-11-19 |
Family
ID=23020582
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP020100370A AR032653A1 (es) | 2001-02-09 | 2002-02-04 | Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos. |
Country Status (7)
Country | Link |
---|---|
US (1) | US6894054B2 (es) |
EP (1) | EP1357913A1 (es) |
JP (1) | JP2004522761A (es) |
AR (1) | AR032653A1 (es) |
AU (1) | AU2002247098B2 (es) |
CA (1) | CA2436079A1 (es) |
WO (1) | WO2002064135A1 (es) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2842804B1 (fr) * | 2002-07-29 | 2004-09-03 | Sanofi Synthelabo | Derives de n-[phenyl(piperidin-2-yl)methyl]benzamide, leur preparation et leur application en therapeutique |
CA2523585A1 (en) * | 2003-04-30 | 2004-11-11 | H. Lundbeck A/S | Aromatic oxyphenyl and aromatic sulfanylphenyl derivatives |
US7202269B2 (en) | 2003-10-30 | 2007-04-10 | Janssen Pharmaceutica N.V. | GlyT2 modulators |
WO2005090320A2 (en) * | 2004-03-12 | 2005-09-29 | Wyeth | Triazole derivatives and method of using the same to treat hiv infections |
CA2583217C (en) * | 2004-10-18 | 2011-05-31 | Amgen Inc. | 1,3,4-thiadiazole compounds as protein kinase inhibitors |
KR100895752B1 (ko) * | 2005-01-07 | 2009-04-30 | 에프. 호프만-라 로슈 아게 | 신경 질환 및 신경정신 질환을 치료하기 위한 글라이신수송자 1(glyt-1) 저해제로서의[4-(헤테로아릴)피페라진-1-일]-(2,5-치환-페닐)메탄온유도체 |
US7514566B2 (en) * | 2006-01-18 | 2009-04-07 | Amgen, Inc. | Thiazole compounds and methods of use |
CA2667545A1 (en) * | 2006-10-25 | 2008-05-02 | Neurosearch A/S | Oxadiazole and thiadiazole compounds and their use as nicotinic acetylcholine receptor modulators |
WO2009011880A2 (en) | 2007-07-17 | 2009-01-22 | Amgen Inc. | Heterocyclic modulators of pkb |
WO2009011871A2 (en) * | 2007-07-17 | 2009-01-22 | Amgen Inc. | Thiadiazole modulators of pkb |
EP2757881A4 (en) * | 2011-09-15 | 2014-11-12 | Univ Kansas | KAPPA OPIOID RECEPTOR EFFECTORS AND USES THEREOF |
CN103373993B (zh) * | 2012-04-12 | 2016-03-02 | 南京大学 | 一类含吡嗪环的噻二唑衍生物及其制法与用途 |
CZ305680B6 (cs) * | 2013-04-04 | 2016-02-03 | Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové | Substituovaný diazol, jeho použití a farmaceutický přípravek ho obsahující |
EP3210469A1 (de) | 2016-02-23 | 2017-08-30 | Bayer Cropscience AG | Verwendung von substituierten thio-1,2,4-triazolen zur steigerung der stresstoleranz in pflanzen |
Family Cites Families (30)
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DE2533605A1 (de) * | 1975-07-26 | 1977-02-03 | Bayer Ag | Antiparasitenmittel |
US4325959A (en) * | 1979-08-09 | 1982-04-20 | The Dow Chemical Company | Hypoglycemic 4-(((1,3,4, thiadiazolyl)thio)methyl)benzoic acids, ester and amides |
DE3031191A1 (de) | 1979-08-21 | 1981-03-12 | CIBA-GEIGY AG, CH 4002 Basel | 1,2,4-triazole mit pestizider wirkung |
US4803211A (en) | 1985-07-22 | 1989-02-07 | Yamanouchi Pharmaceutical Co., Ltd. | Thiadizazole compounds as antagonists of SRS-A |
US4900743A (en) | 1987-01-27 | 1990-02-13 | Merrell Dow Pharmaceuticals Inc. | 3-aryl-5-alkylthio-4H-1,2,4-triazoles |
DE3717865A1 (de) | 1987-05-26 | 1988-12-15 | Schering Ag | Neue 1,2,4-triazolderivate, verfahren zur herstellung dieser verbindungen sowie diese enthaltende akarizide und insektizide mittel |
JPH02129173A (ja) | 1988-11-10 | 1990-05-17 | Ishihara Sangyo Kaisha Ltd | トリアゾール系化合物、それらの製造方法及びそれらを含有する有害生物防除剤 |
EP0409332A3 (en) | 1989-07-19 | 1991-08-07 | Merck & Co. Inc. | Substituted triazoles as angiotensin ii antagonists |
JP2726563B2 (ja) | 1990-02-13 | 1998-03-11 | メルク・エンド・カムパニー・インコーポレーテツド | 置換ベンジル要素を含むトリアゾールアンギオテンシン▲ii▼拮抗物質 |
CA2123323A1 (en) * | 1991-11-12 | 1993-05-27 | Neurogenetic Corporation | Dna encoding a glycine transporter and uses thereof |
US6127131A (en) * | 1991-11-12 | 2000-10-03 | Synaptic Pharmaceutical Corporation | DNA encoding a glycine transporter and uses thereof |
GB2263635A (en) | 1992-01-28 | 1993-08-04 | Merck & Co Inc | Substitiuted triazoles as neurotensin antagonists |
US5240953A (en) | 1992-01-30 | 1993-08-31 | Ortho Pharmaceutical Corporation | Substituted triazoles as angiotensin ii inhibitors |
JPH075646A (ja) | 1993-06-17 | 1995-01-10 | Konica Corp | ハロゲン化銀カラー写真感光材料 |
AU5533394A (en) | 1993-11-12 | 1995-05-29 | Gyogyszerkutato Intezet Kft | Ulcer-inhibiting triazole derivatives, pharmaceutical compositions containing them and process for preparing same |
US5587293A (en) * | 1994-01-06 | 1996-12-24 | Terrapin Technologies, Inc. | Method to identify binding partners |
JPH09114055A (ja) | 1995-10-18 | 1997-05-02 | Konica Corp | ハロゲン化銀カラー写真感光材料 |
US5670526A (en) * | 1995-12-21 | 1997-09-23 | Otsuka Pharmaceutical Co., Ltd. | 1,3,4-oxadiazoles |
US5668159A (en) * | 1996-05-08 | 1997-09-16 | The Dupont Merck Pharmaceutical Company | 1,3,4-thiadiazoles and 1,3,4-oxadiazoles as IIb/IIIa antagonists |
AU737095B2 (en) | 1996-05-31 | 2001-08-09 | Nps Pharmaceuticals, Inc. | Pharmaceutical for treating of neurological and neuropsychiatric disorders |
US5824486A (en) * | 1996-05-31 | 1998-10-20 | Allelix Neuroscience Inc. | Glycine transporter-transfected cells and uses thereof |
CA2254833C (en) | 1996-05-31 | 2008-04-29 | Allelix Neuroscience Inc. | Pharmaceutical for treatment of neurological and neuropsychiatric disorders |
JPH1036357A (ja) | 1996-07-25 | 1998-02-10 | Mitsubishi Kagaku Kk | トリアゾール誘導体並びにそれを含有する農園芸用殺菌剤 |
US6191152B1 (en) | 1997-01-14 | 2001-02-20 | Egis Gyógyszergyar Rt. | 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives having an effect on the C.N.S. and the heart |
US6008015A (en) * | 1997-04-11 | 1999-12-28 | Allelix Neuroscience Inc. | Glycine transporter |
JP4151087B2 (ja) | 1997-07-28 | 2008-09-17 | チッソ株式会社 | スルフェニルチアジアゾール誘導体およびチアジアゾールチオエステル誘導体 |
PL343435A1 (en) | 1998-03-06 | 2001-08-13 | Janssen Pharmaceutica Nv | Glycine transport inhibitors |
WO1999045011A1 (en) | 1998-03-06 | 1999-09-10 | Janssen Pharmaceutica N.V. | Glycine transport inhibitors |
GB0002666D0 (en) | 2000-02-04 | 2000-03-29 | Univ London | Blockade of voltage dependent sodium channels |
HUP0302415A2 (hu) | 2000-05-19 | 2003-11-28 | Merck Patent Gmbh | Triazolszármazékokat tartalmazó gyógyszerkészítmények és új triazolszármazékok |
-
2002
- 2002-02-04 AR ARP020100370A patent/AR032653A1/es unknown
- 2002-02-05 US US10/072,308 patent/US6894054B2/en not_active Expired - Fee Related
- 2002-02-08 CA CA002436079A patent/CA2436079A1/en not_active Abandoned
- 2002-02-08 EP EP02714858A patent/EP1357913A1/en not_active Withdrawn
- 2002-02-08 AU AU2002247098A patent/AU2002247098B2/en not_active Ceased
- 2002-02-08 JP JP2002563929A patent/JP2004522761A/ja not_active Withdrawn
- 2002-02-08 WO PCT/US2002/003837 patent/WO2002064135A1/en active Application Filing
Also Published As
Publication number | Publication date |
---|---|
WO2002064135A1 (en) | 2002-08-22 |
CA2436079A1 (en) | 2002-08-22 |
EP1357913A1 (en) | 2003-11-05 |
JP2004522761A (ja) | 2004-07-29 |
AU2002247098B2 (en) | 2006-06-22 |
US6894054B2 (en) | 2005-05-17 |
US20030073726A1 (en) | 2003-04-17 |
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