AR088921A2 - PROCESO PARA LA PREPARACION DE DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTA mGluR5, COMPOSICIONES Y USO DE LOS COMPUESTOS - Google Patents
PROCESO PARA LA PREPARACION DE DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTA mGluR5, COMPOSICIONES Y USO DE LOS COMPUESTOSInfo
- Publication number
- AR088921A2 AR088921A2 ARP120104356A ARP120104356A AR088921A2 AR 088921 A2 AR088921 A2 AR 088921A2 AR P120104356 A ARP120104356 A AR P120104356A AR P120104356 A ARP120104356 A AR P120104356A AR 088921 A2 AR088921 A2 AR 088921A2
- Authority
- AR
- Argentina
- Prior art keywords
- hydrogen
- alkyl
- formula
- compound
- preparation
- Prior art date
Links
Classifications
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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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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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
- A61P25/04—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
- A61P25/22—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
- A61P25/32—Alcohol-abuse
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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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
- C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/20—Oxygen atoms
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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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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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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- 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
- C07D405/06—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 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
Abstract
Proceso para la preparación de derivados de acetileno que tienen actividad antagonista mGIuR5. Composición farmacéutica que lo comprende. Reivindicación 1: Un proceso para la preparación de un compuesto de la fórmula (1), en la que: m es 0 ó 1; n es 0 ó 1; y A es hidroxi; X es hidrógeno, e Y es hidrógeno; o A forma una ligadura simple con X o con Y; R⁰ es hidrógeno, alquilo C₁₋₄, alcoxi C₁₋₄, trifluorometilo, halógeno, ciano, nitro, -COOR¹; donde R¹ es alquilo C₁₋₄, o -COR², donde R² es hidrógeno o alquilo C₁₋₄; y R es -COR³, -COOR³, -CONR⁴R⁵ ó -SO₂R⁶; donde R³ es alquilo C₁₋₄, cicloalquilo C₃₋₇ o fenilo opcionalmente sustituido, 2-piridilo o 2-tienilo; R⁴ y R⁵, independientemente, son hidrógeno o alquilo C₁₋₄ y R⁶ es alquilo C₁₋₄, cicloalquilo C₃₋₇ o fenilo opcionalmente sustituido; R es hidrógeno o alquilo C₁₋₄; y R es hidrógeno o alquilo C₁₋₄; o R y R forman juntos un grupo -CH₂(CH₂)ₚ-; donde p es 0, 1 ó 2; en cuyo caso uno de n y p es diferente de 0; a condición de que R⁰ sea diferente de hidrógeno, trifluorometilo y metoxi cuando m es 1, n es 0, A es hidroxi, X e Y son ambos hidrógeno, R es COOEt y R y R forman juntos un grupo -(CH₂)₂-; en forma de base libre o de una sal de adición de ácido, caracterizado porque comprende el paso de: a) para la producción de un compuesto de la fórmula (1), en la que A es hidroxi, hacer reaccionar un compuesto de la fórmula (2) en la que m, n, R, R y R son como se definió en la reivindicación 1, con un compuesto de la fórmula (3) en la que R⁰ es como se definió en la reivindicación 1; o b) para la producción de un compuesto de la fórmula (1) en el que A forma una ligadura simple con X o con Y, deshidratar un compuesto de la fórmula (1) en la que A es hidroxi; y recuperar el compuesto resultante de la fórmula (1), en forma de la base libre o de una sal de adición de ácido.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0128996.6A GB0128996D0 (en) | 2001-12-04 | 2001-12-04 | Organic compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
AR088921A2 true AR088921A2 (es) | 2014-07-16 |
Family
ID=9926969
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP020104641A AR037682A1 (es) | 2001-12-04 | 2002-12-02 | Derivados de acetileno que tienen actividad antagonista para receptores glutamato metabotropico humanos, composicion farmaceutica, una combinacion y el uso de dichos derivados para la fabricacion de composiciones farmaceuticas |
ARP120104356A AR088921A2 (es) | 2001-12-04 | 2012-11-20 | PROCESO PARA LA PREPARACION DE DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTA mGluR5, COMPOSICIONES Y USO DE LOS COMPUESTOS |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP020104641A AR037682A1 (es) | 2001-12-04 | 2002-12-02 | Derivados de acetileno que tienen actividad antagonista para receptores glutamato metabotropico humanos, composicion farmaceutica, una combinacion y el uso de dichos derivados para la fabricacion de composiciones farmaceuticas |
Country Status (32)
Country | Link |
---|---|
US (4) | US7348353B2 (es) |
EP (1) | EP1453512B8 (es) |
JP (2) | JP4176020B2 (es) |
KR (2) | KR100959204B1 (es) |
CN (2) | CN100430059C (es) |
AR (2) | AR037682A1 (es) |
AT (1) | ATE327755T1 (es) |
AU (1) | AU2002358585B2 (es) |
BR (1) | BR0214666A (es) |
CA (1) | CA2466560C (es) |
CO (1) | CO5590929A2 (es) |
CY (1) | CY1105460T1 (es) |
DE (1) | DE60211944T2 (es) |
DK (1) | DK1453512T3 (es) |
EC (1) | ECSP045139A (es) |
EG (1) | EG24936A (es) |
ES (1) | ES2263842T3 (es) |
GB (1) | GB0128996D0 (es) |
HK (1) | HK1071510A1 (es) |
HU (1) | HU229429B1 (es) |
IL (1) | IL161990A0 (es) |
MX (1) | MXPA04005456A (es) |
MY (1) | MY137774A (es) |
NO (1) | NO327005B1 (es) |
NZ (1) | NZ533266A (es) |
PE (1) | PE20030640A1 (es) |
PL (1) | PL212996B1 (es) |
PT (1) | PT1453512E (es) |
RU (1) | RU2341515C2 (es) |
TW (1) | TWI328578B (es) |
WO (1) | WO2003047581A1 (es) |
ZA (1) | ZA200403713B (es) |
Families Citing this family (44)
Publication number | Priority date | Publication date | Assignee | Title |
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GB0128996D0 (en) | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
GB0325956D0 (en) * | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
GB0508318D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0508314D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0508319D0 (en) | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0514296D0 (en) * | 2005-07-12 | 2005-08-17 | Novartis Ag | Organic compounds |
WO2008031550A2 (en) * | 2006-09-11 | 2008-03-20 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutanate receptors |
WO2008151257A2 (en) | 2007-06-04 | 2008-12-11 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
AU2012254934B2 (en) * | 2007-10-12 | 2013-10-17 | Novartis Ag | Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease |
US20100249136A1 (en) * | 2007-10-12 | 2010-09-30 | Daniel Umbricht | Organic compounds |
WO2009149279A2 (en) | 2008-06-04 | 2009-12-10 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
US8703809B2 (en) * | 2008-06-30 | 2014-04-22 | Novartis Ag | Combination products |
WO2010018154A1 (en) * | 2008-08-12 | 2010-02-18 | Novartis Ag | Processes for the preparation of 4-oxo-octahydro-indole-1-carbocylic acid methyl ester and derivatives thereof |
US8334287B2 (en) | 2009-07-17 | 2012-12-18 | Hoffmann-La Roche Inc. | Imidazoles |
CN102573842A (zh) | 2009-07-23 | 2012-07-11 | 诺瓦提斯公司 | 氮杂双环烷基衍生物或吡咯烷-2-酮衍生物的用途 |
JO3250B1 (ar) | 2009-09-22 | 2018-09-16 | Novartis Ag | إستعمال منشطات مستقبل نيكوتينيك أسيتيل كولين ألفا 7 |
EP2490691A1 (en) | 2009-10-20 | 2012-08-29 | Novartis AG | Use of 1h-quinazoline-2,4-diones |
MA34263B1 (fr) * | 2010-04-30 | 2013-05-02 | Novartis Ag | Marqueurs de prédiction utiles dans traitement du syndrome de l'x fragile (fxs) |
MX2012015090A (es) | 2010-06-24 | 2013-02-12 | Novartis Ag | Uso de 1h-quinazolina-2,4-dionas. |
US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
WO2012084873A1 (en) | 2010-12-20 | 2012-06-28 | Novartis Ag | 4- (hetero) aryl - ethynyl - octahydro - indole - 1 - carboxylic acid esters |
US9067881B2 (en) | 2011-01-24 | 2015-06-30 | Novartis Ag | 4-tolyl-ethynyl-octahydro-indole-1-ester derivatives |
BR112013018726A2 (pt) | 2011-01-27 | 2016-10-25 | Novartis Ag | uso de ativadores de alfa 7 do receptor nicotínico de acetilcolina |
US20140228398A1 (en) | 2011-03-18 | 2014-08-14 | Novartis Ag | COMBINATIONS OF ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR ACTIVATORS AND mGluR5 ANTAGONISTS FOR USE IN DOPAMINE INDUCED DYSKINESIA IN PARKINSON'S DISEASE |
IN2014DN01791A (es) | 2011-09-07 | 2015-05-15 | Novartis Ag | |
WO2013131981A1 (en) | 2012-03-08 | 2013-09-12 | Novartis Ag | Predictive markers useful in the diagnosis and treatment of fragile x syndrome (fxs) |
GB201215033D0 (en) | 2012-08-23 | 2012-10-10 | Novartis Ag | Diazepinone derivatives |
ES2865736T3 (es) | 2013-01-15 | 2021-10-15 | Novartis Ag | Uso de agonistas del receptor de acetilcolina nicotínico alfa 7 |
CA2898043C (en) | 2013-01-15 | 2019-08-06 | Novartis Ag | Use of alpha 7 nicotinic receptor agonists for the treatment of narcolepsy |
EP2968439A2 (en) | 2013-03-15 | 2016-01-20 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
JP2016514671A (ja) | 2013-03-15 | 2016-05-23 | シナジー ファーマシューティカルズ インコーポレイテッド | グアニル酸シクラーゼのアゴニストおよびその使用 |
CA2913737A1 (en) | 2013-06-05 | 2014-12-11 | Synergy Pharmaceuticals, Inc. | Ultra-pure agonists of guanylate cyclase c, method of making and using same |
CN105263479A (zh) | 2013-06-12 | 2016-01-20 | 诺华股份有限公司 | 调整释放制剂 |
CN105669686B (zh) * | 2014-11-19 | 2018-08-03 | 上海合全药业股份有限公司 | 一种6-(叔丁氧羰基)八氢呋喃[2,3-c]吡啶-4-羧酸的合成方法 |
US11878001B2 (en) | 2017-07-31 | 2024-01-23 | Novartis Ag | Use of mavoglurant in the reduction of ***e use or in preventing relapse into ***e use |
CN110891564A (zh) | 2017-07-31 | 2020-03-17 | 诺华股份有限公司 | 玛沃谷兰在减少酒精使用或在预防复用酒精中的用途 |
WO2020157640A1 (en) | 2019-01-29 | 2020-08-06 | Novartis Ag | The use of an mglur5 antagonist for treating opioid analgesic tolerance |
BR112022025730A2 (pt) | 2020-07-17 | 2023-01-24 | Novartis Ag | Uso de antagonistas de mglur5 |
CN116710084A (zh) | 2020-12-11 | 2023-09-05 | 诺华股份有限公司 | mGluR5拮抗剂用于治疗***成瘾的用途 |
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KR20050044660A (ko) | 2001-12-04 | 2005-05-12 | 에프. 호프만-라 로슈 아게 | 치환된 2-아미노-사이클로알칸카복스아마이드 및 시스테인프로테아제 저해제로서의 이의 용도 |
GB0128996D0 (en) * | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
TW200303309A (en) | 2001-12-04 | 2003-09-01 | Bristol Myers Squibb Co | Novel n-[4-(1h-imidazol-1-yl)-2-fluorophenyl]-3-trifluoromethyl)-1h-pyrazole-5-carboxamides as factor Xa inhibitors |
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