AR043469A1 - Compuestos arilvinilazacicloalcano y composiciones farmaceuticas que los contienen - Google Patents
Compuestos arilvinilazacicloalcano y composiciones farmaceuticas que los contienenInfo
- Publication number
- AR043469A1 AR043469A1 ARP040100690A ARP040100690A AR043469A1 AR 043469 A1 AR043469 A1 AR 043469A1 AR P040100690 A ARP040100690 A AR P040100690A AR P040100690 A ARP040100690 A AR P040100690A AR 043469 A1 AR043469 A1 AR 043469A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- heteroaryl
- aryl
- cycloalkyl
- Prior art date
Links
Classifications
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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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- C07D401/06—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 only aliphatic carbon atoms
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- 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
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
- A61P1/12—Antidiarrhoeals
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- 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
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- 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
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- 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
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- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
- A61P25/34—Tobacco-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- 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
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- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
- C07D403/06—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 only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychology (AREA)
- Immunology (AREA)
- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a compuestos arilvinilazacicloalcano y composiciones farmacéuticas que los contienen. Método de preparación de dichos compuestos que comprende la reacción de un aldehído con un iluro de fosforano, para dar un vinilazacicloalcano, su reacción con haluro de heteroarilo y remoción de los grupos protectores remanentes. Su uso para prevenir o tratar trastornos neurovegetativos, asociados con la disfunción nAChRs, especialmente en el sistema nervioso central o gastrointestinal, tales como enfermedad de Alzheimer, de Parkinson, inflamatorios, adicción a drogas, dolores, etc., evitando efectos indeseables en tejidos periféricos. Reivindicación 1: Un compuesto de la fórmula (1) en donde la línea ondulante representa la geometría variable (E o Z) alrededor del enlace doble; X es N o C-R2; R1 es H, alquilo de C1-6, halógeno, -OR4, -NR4R5, o -SR4 cuando X es C-R2 e H, alquilo de C1-6, -OR4, o -NR4R5 cuando X es N; R2 es H, alquilo de C1-6, arilo, aril-alquilo de C1-6, alquil-arilo de C1-6, heteroarilo, heteroaril-alquilo de C1-6, heterociclilo, heterociclilalquilo, cicloalquilo, policicloalquilo, -OR6, -NR6R7, -SR6, -SOR6, o -SO2R6, cada uno de los cuales puede optativamente sustituirse con 1 o más sustituyentes que se seleccionan de halógeno, -CN, -NO2, -NH2, -OH, OR6, -COOH, -C(O)OR6, -O-C(O)R6, -NR6R7, -NHC(O)R6, -C(O)NR6R7, -SR6, -S(O)R6, -SO2R6, -NHSO2R6, -SO2NR6R6, -C(S)NR6R6, -NHC(S)R6, -O-SO2R6, arilo, heteroarilo, formilo, trifluorometilo, trifluorometilsulfanilo, trifluorometoxi y alquilo de C1-6; R3 es H, alquilo de C1-6, aril alquilo de C1-6, heteroaril alquilo de C1-6, heterociclilo, heterociclilalquilo, cicloalquilo o policicloalquilo; m es entre 1 y 4; n es entre 1 y 3; R4 y R5 son, independientemente, H o alquilo de C1-6-; R6 y R7 son, independientemente, H, alquilo de C1-6 ( que incluye cicloalquilo que contiene alquilo), arilo, aril-alquilo de C1-6, heteroarilo, heteroaril-alquilo de C1-6, heterociclilo, heterocicloalquilo, cicloalquilo o policicloalquilo, cada uno de los cuales puede optativamente ser sustituido con uno o más sustituyentes que se seleccionan de halógeno, alquilo de C1-6, alcoxi de C1-6, -CN, -NO2, -NH2, -OH, -COOH, -COO-alquilo de C1-6, -CONH2, formilo, trifluorometilo y trifluorometoxi, en donde los grupos alquilo de C1-6, heterocíclicos, heteroarilo y arilo pueden sustituirse con 1-6 sustituyentes que se seleccionan del grupo formado por F, Cl, Br, I, R8, -NR8R9, -CF3, -CN, -NO2, -C2R8, -N3, -SO2CH3, -OR8, -SR8, -C(=O)NR8R9, -NR8C(=O)R8, -C(=O)R8, -C(=O)OR8, -(CH2)qOR8, -OC(=O)R8, -OC(=O)NR8R9 y -NR8C(=O)OR8, donde R8 y R9 son individualmente, alquilo de C1-6, piridilo, piridilo sustituido, quinolinilo, quinolinilo sustituido, pirimidinilo, pirimidinilo sustituido, fenilo, fenilo sustituido, bencilo, o bencilo sustituido ( sustituidos con uno o más de los sustituyentes precedentes), y en donde R6 y R7 o R8 y R9 pueden formar una funcionalidad cicloalquilo de C1-10, e isómeros, mezclas, enantiómeros, diastereómeros, tautómeros, y sales farmacéuticamente aceptables de ellos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/379,868 US7098331B2 (en) | 2003-03-05 | 2003-03-05 | Arylvinylazacycloalkane compounds and methods of preparation and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR043469A1 true AR043469A1 (es) | 2005-07-27 |
Family
ID=32926772
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040100690A AR043469A1 (es) | 2003-03-05 | 2004-03-04 | Compuestos arilvinilazacicloalcano y composiciones farmaceuticas que los contienen |
| ARP090100388A AR070569A2 (es) | 2003-03-05 | 2009-02-05 | Compuestos de arilvinilazacicloalcano, composiciones farmaceuticas que los comprenden, un proceso para prepararlos y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurodegenerativos. |
| ARP090100389A AR070570A2 (es) | 2003-03-05 | 2009-02-05 | Compuesto de arilvinilazacicloalcano, una composicion farmaceutica que lo comprende y su uso en el tratamiento de enfermedades mediadas por alfa4beta2 nachr. |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100388A AR070569A2 (es) | 2003-03-05 | 2009-02-05 | Compuestos de arilvinilazacicloalcano, composiciones farmaceuticas que los comprenden, un proceso para prepararlos y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurodegenerativos. |
| ARP090100389A AR070570A2 (es) | 2003-03-05 | 2009-02-05 | Compuesto de arilvinilazacicloalcano, una composicion farmaceutica que lo comprende y su uso en el tratamiento de enfermedades mediadas por alfa4beta2 nachr. |
Country Status (32)
| Country | Link |
|---|---|
| US (8) | US7098331B2 (es) |
| EP (3) | EP1601670B1 (es) |
| JP (3) | JP4663627B2 (es) |
| KR (4) | KR101018083B1 (es) |
| CN (3) | CN101255155A (es) |
| AR (3) | AR043469A1 (es) |
| AT (3) | ATE496046T1 (es) |
| AU (3) | AU2004217903B2 (es) |
| BR (1) | BRPI0409576A (es) |
| CA (1) | CA2516514C (es) |
| CL (1) | CL2004000452A1 (es) |
| CY (2) | CY1110391T1 (es) |
| DE (2) | DE602004013553D1 (es) |
| DK (2) | DK2085395T3 (es) |
| EA (3) | EA019240B1 (es) |
| ES (3) | ES2389106T3 (es) |
| GT (1) | GT200400033A (es) |
| HK (3) | HK1084949A1 (es) |
| IL (3) | IL170155A (es) |
| JO (1) | JO2488B1 (es) |
| MX (1) | MXPA05009386A (es) |
| NO (3) | NO331920B1 (es) |
| NZ (1) | NZ541795A (es) |
| PA (1) | PA8597201A1 (es) |
| PE (1) | PE20040930A1 (es) |
| PL (5) | PL215059B1 (es) |
| PT (2) | PT2085395E (es) |
| SI (2) | SI1601670T1 (es) |
| TW (3) | TWI339662B (es) |
| UY (1) | UY28218A1 (es) |
| WO (1) | WO2004078752A1 (es) |
| ZA (1) | ZA200506790B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7098331B2 (en) * | 2003-03-05 | 2006-08-29 | Targacept, Inc. | Arylvinylazacycloalkane compounds and methods of preparation and use thereof |
| FR2896800B1 (fr) * | 2006-01-30 | 2008-04-11 | Servier Lab | Nouveaux composes pyridinylaminoalkylene-et pyridinyloxyalkylene-cyclopropanamines polysubstitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| WO2008157365A2 (en) * | 2007-06-15 | 2008-12-24 | Targacept, Inc. | Vinylazacycloalkanes for treating neuropathic pain |
| US20110098312A1 (en) * | 2008-05-12 | 2011-04-28 | Targacept ,Inc | Methods for preventing the development of retinopathy by the oral administration of nnr ligands |
| US8604191B2 (en) * | 2008-12-01 | 2013-12-10 | Targacept, Inc. | Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3YLVINYL)pyrimidine |
| US9145396B2 (en) | 2008-12-01 | 2015-09-29 | Targacept, Inc. | Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine |
| TW201024283A (en) * | 2008-12-01 | 2010-07-01 | Targacept Inc | Synthesis and novel salt forms of (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine |
| WO2010080757A2 (en) | 2009-01-07 | 2010-07-15 | Astrazeneca Ab | Combinations with an alpha-4beta-2 nicotinic agonist |
| KR20120061047A (ko) * | 2009-06-17 | 2012-06-12 | 타가셉트 인코포레이티드 | 신경원성 니코틴 수용체 리간드에 의한 ｌ?도파?유도 운동 장애의 역전 |
| WO2011071758A1 (en) | 2009-12-07 | 2011-06-16 | Targacept, Inc. | 3,6-diazabicyclo[3.1.1]heptanes as neuronal nicotinic acetylcholine receptor ligands |
| MX2012010491A (es) * | 2010-03-11 | 2013-01-25 | Targacept Inc | Compuestos arilvinilazacicloalcano para la constipacion. |
| US20110274628A1 (en) * | 2010-05-07 | 2011-11-10 | Borschke August J | Nicotine-containing pharmaceutical compositions |
| US20140081714A1 (en) * | 2012-09-19 | 2014-03-20 | Salesforce.Com, Inc. | Systems and methods of rewarding users in an on-demand system |
| US20140278929A1 (en) * | 2013-03-15 | 2014-09-18 | Yahoo! Inc. | System and method identifying opportunities for advertising entities based on user goal achievement |
| CN114432313A (zh) | 2016-04-07 | 2022-05-06 | 奥伊斯特普安生物制药公司 | 治疗眼部病状的方法 |
| KR101848601B1 (ko) * | 2016-07-27 | 2018-04-12 | 송기봉 | 일회용 위생 티슈 |
| CN112638364A (zh) | 2018-07-10 | 2021-04-09 | 奥伊斯特普安生物制药公司 | 用于治疗眼部病症的正向别构调节剂和烟碱型乙酰胆碱受体激动剂的组合 |
| WO2020014217A1 (en) | 2018-07-10 | 2020-01-16 | Oyster Point Pharma, Inc. | Methods of treating ocular conditions |
| EP4142734A1 (en) | 2020-04-28 | 2023-03-08 | Oyster Point Pharma, Inc. | Local administration of nicotinic acetylcholine receptor agonists for the inhibition of coronavirus infections |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1989000158A1 (en) | 1987-07-02 | 1989-01-12 | Pfizer Inc. | Bridged-diazabicycloalkyl quinolone carboxylic acids and esters |
| US4922901A (en) * | 1988-09-08 | 1990-05-08 | R. J. Reynolds Tobacco Company | Drug delivery articles utilizing electrical energy |
| US5187166A (en) * | 1990-07-31 | 1993-02-16 | Nisshin Flour Milling Co., Ltd. | Azabicyclo derivatives and their use as antiemetics |
| IL107184A (en) | 1992-10-09 | 1997-08-14 | Abbott Lab | Heterocyclic ether compounds that enhance cognitive function |
| US5852041A (en) * | 1993-04-07 | 1998-12-22 | Sibia Neurosciences, Inc. | Substituted pyridines useful as modulators of acethylcholine receptors |
| IT1274018B (it) * | 1994-02-23 | 1997-07-14 | Riace Ets | Derivati del 3,8-diazabiciclo(3.2.1.)ottano ad attivita' analgesica |
| GB2295387A (en) | 1994-11-23 | 1996-05-29 | Glaxo Inc | Quinazoline antagonists of alpha 1c adrenergic receptors |
| US5597919A (en) * | 1995-01-06 | 1997-01-28 | Dull; Gary M. | Pyrimidinyl or Pyridinyl alkenyl amine compounds |
| US5604231A (en) * | 1995-01-06 | 1997-02-18 | Smith; Carr J. | Pharmaceutical compositions for prevention and treatment of ulcerative colitis |
| US5585388A (en) * | 1995-04-07 | 1996-12-17 | Sibia Neurosciences, Inc. | Substituted pyridines useful as modulators of acetylcholine receptors |
| US5583140A (en) * | 1995-05-17 | 1996-12-10 | Bencherif; Merouane | Pharmaceutical compositions for the treatment of central nervous system disorders |
| IL118279A (en) | 1995-06-07 | 2006-10-05 | Abbott Lab | Compounds 3 - Pyridyloxy (or Thio) Alkyl Heterocyclic Pharmaceutical Compositions Containing Them and Their Uses for Preparing Drugs to Control Synaptic Chemical Transmission |
| US5616716A (en) * | 1996-01-06 | 1997-04-01 | Dull; Gary M. | (3-(5-ethoxypyridin)yl)-alkenyl 1 amine compounds |
| AT403803B (de) | 1996-04-19 | 1998-05-25 | Sanochemia Ltd | Neue benzazepinderivate, diese enthaltende arzneimittel und verwendung derselben zum herstellen von arzneimitteln |
| US5663356A (en) * | 1996-04-23 | 1997-09-02 | Ruecroft; Graham | Method for preparation of aryl substituted alefinic secondary amino compounds |
| US6437138B1 (en) * | 1996-06-06 | 2002-08-20 | Abbott Laboratories | 3-pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission |
| US5629325A (en) | 1996-06-06 | 1997-05-13 | Abbott Laboratories | 3-pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission |
| WO1999021834A1 (en) | 1997-10-27 | 1999-05-06 | Neurosearch A/S | Heteroaryl diazacycloalkanes as cholinergic ligands at nicotinic acetylcholine receptors |
| WO2000075110A1 (en) | 1999-06-07 | 2000-12-14 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
| JP2003529547A (ja) | 1999-09-14 | 2003-10-07 | アボット・ラボラトリーズ | 化学シナプス伝達のコントロールに有効な３−ピロリジニルオキシ−３’−ピリジルエーテル化合物 |
| AU780492B2 (en) | 1999-11-01 | 2005-03-24 | Targacept, Inc. | Aryl olefinic azacyclic, and aryl acetylenic azacyclic compounds, pharmaceutical compositions containing them and their use as inhibitors of nicotinic cholinergic receptors |
| US6624167B1 (en) * | 2000-08-04 | 2003-09-23 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
| US6881738B2 (en) | 2001-07-19 | 2005-04-19 | Medical College Of Georgia Research Institute | Analogs of choline for neuroprotection and cognitive enhancement in neurodegenerative disorders |
| US7098331B2 (en) * | 2003-03-05 | 2006-08-29 | Targacept, Inc. | Arylvinylazacycloalkane compounds and methods of preparation and use thereof |
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