AR078126A1 - Antagonistas de glicina b, composiciones farmaceuticas, usos y proceso de preparacion de los mismos - Google Patents
Antagonistas de glicina b, composiciones farmaceuticas, usos y proceso de preparacion de los mismosInfo
- Publication number
- AR078126A1 AR078126A1 ARP100101979A ARP100101979A AR078126A1 AR 078126 A1 AR078126 A1 AR 078126A1 AR P100101979 A ARP100101979 A AR P100101979A AR P100101979 A ARP100101979 A AR P100101979A AR 078126 A1 AR078126 A1 AR 078126A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- 6alkyl
- aryl
- heteroaryl
- 6alkoxy
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
- C07C311/51—Y being a hydrogen or a carbon atom
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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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
- C07C235/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
- C07C235/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atom of at least one of the carboxamide 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
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
- C07C235/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
- C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/16—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound oxygen atoms bound to the same carbon atom of an acyclic carbon skeleton
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- C07C255/00—Carboxylic acid nitriles
- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
- C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
- C07C255/44—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
- C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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- C—CHEMISTRY; METALLURGY
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- 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
- C07C271/20—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 nitrogen atoms not being part of nitro or nitroso groups
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- C—CHEMISTRY; METALLURGY
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
- C07C49/84—Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/21—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
- C07C65/24—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
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- 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
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
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- C07D215/06—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 having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
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Abstract
Derivados de naftaleno y sus sales farmacéuticamente aceptables y proceso para la preparacion de dichos compuestos. Los compuestos de la solicitud son antagonistas de glicina B y por lo tanto son utiles para el control y prevencion de diferentes trastornos, incluyendo trastornos neurologicos. Reivindicacion 1: Un compuesto caracterizado porque se selecciona entre los de la formula (1) donde R1 representa hidrogeno, halogeno, nitro, acilamino, trifluorometilo, alquilo C1-6, alcoxi C1-6, hidroxi-C1-6alquilo, o alcoxi C1-6-alquilo C1-6; R2 representa hidrogeno, halogeno, nitro, trifluorometilo, alquilo C1-6, o alcoxi C1-6; R3 representa halogeno, nitro, trifluorometilo, o alquilo C1-6; R4 representa hidrogeno, CONH2, aIquilo C1-6, alquenilo C3-6, alquinilo C3-6, hidroxi-C1-6alquilo, carboxi-C1-6aIquilo, alcoxi C1-6-alquilo C1-6, carbamoil-C1-6alquilo, arilo, heteroarilo, ciclo-C3-12alquilo, ciclo-C3-12alquil-C1-6alquilo, ciclo-C3-12alcoxi-C1-6alquilo, aril-C1-6alquilo, heteroaril-C1-6alquilo, ariloxi-C1-6alquilo, heteroariloxi-C1-6alquilo, aril-C1-6aIcoxi-C1-6alquilo, heteroaril-C1-6aIcoxi-C1-6alquilo, arilamino-C1-6alquilo, heteroarilamino-C1-6alquilo, ciclo-C3-12alquil-amino-C1-6alquilo, alquilaminocarbonil C1-6-alquilo C1-6, ciclo-C3-12alquilaminocarbonil-C1-6alquilo, arilaminocarbonil-C1-6alquilo, heteroarilaminocarbonil-C1-6aIquilo, carboxi-C1-6alquilamino-C1-6alquilo, acilamino-C1-6aIquilo; arilsulfonilamino-C1-6alquilo, alquilsulfonilamino C1-6-alquilo C1-6, ciclo-C3-12aIquil-C1-6alquilaminocarbonil-C1-6alquilo, aril-C1-6alquilaminocarbonil-C1-6alquilo, heteroaril-C1-6alquilaminocarbonil-C1-6alquilo, hidroxi-C1-6alquilaminocarbonil-C1-6alquilo, di-(alquil C1-6)aminocarbonil-C1-6alquilo, aril(alquil C1-6)aminocarbonil-C1-6alquilo, o heteroaril(alquil C1-6)aminocarbonil-C1-6alquilo; R5 representa hidrogeno o alquilo C1-6; R6 representa hidroxi, alcoxi C1-6, hidroxi-C1-6aIcoxi, arilo, heteroarilo, o NR7R8; R7 y R8, que pueden ser iguales o diferentes, representan en forma independiente entre sí hidrogeno, aIquilo C1-6, alquenilo C3-6, alquinilo C3-6, alquilamino C1-6, arilamino, di(alquil C1-6)amino, aril(alquil C1-6)amino, alcoxicarbonilo C1-6, alquilsulfonilo C1-6, arilsulfonilo, heteroarilsulfonilo, alquil C1-6-carbamoilo, ciclo-3-12alquilaminocarbonilo, arilaminocarbonilo, heteroarilaminocarbonilo, di-(alquil C1-6)aminocarbonilo, aril(alquil C1-6)aminocarbonilo, heteroaril(alquil C1-6)aminocarbonilo, hidroxi-C1-6alquilo, hidroxi(aril)-C1-6aIquilo, carboxi-C1-6alquilo, alcoxicarbonil C1-6-alquilo C1-6, carboxi(aril)-C1-6alquilo, carboxi(aril-C1-6alquil)-C1-6alquilo, alcoxi C1-6-alquilo C1-6, carbamoil-C1-6alquilo, arilo, heteroarilo, ciclo-C3-12alquilo, ciclo-C3-12alquil-C1-6aIquilo, aril-C1-6alquilo, heteroaril-C1-6alquilo, aril-ciclo-C3-12alquilo, heteroaril-ciclo-C3-12alquilo, ciclo-C3-12alcoxi-C1-6alquilo, ariloxi-C1-6alquilo, heteroariloxi-C1-6alquilo, aril-C1-6alcoxi-C1-6aIquilo, heteroaril-C1-6aIcoxi-C1-6aIquilo, arilamino-C1-6alquilo, heteroarilamino-C1-6alquilo, ciclo-C3-12alquilamino-C1-6alquilo, alquilaminocarbonil C1-6-alquilo C1-6, ciclo-C3-12alquilaminocarbonil-C1-6alquilo, arilaminocarbonil-C1-6alquilo, heteroarilaminocarbonil-C1-6aIquilo, carboxi-C1-6alquilamino-C1-6alquilo, acilamino-C1-6aIquilo; aIquilsulfonilamino C1-6-alquilo C1-6, arilsulfonilamino-C1-6alquilo, ciclo-C3-12alquil-C1-6alquilaminocarbonil-C1-6alquilo, aril-C1-6alquilaminocarbonil-C1-6alquilo, heteroaril-C1-6aIquilaminocarbonil-C1-6alquilo, hidroxi-C1-6alquilaminocarbonil-C1-6aIquilo, di-(alquil C1-6)aminocarbonil-C1-6alquilo, aril(alquil C1-6)aminocarbonil-C1-6aIquilo, o heteroaril(alquil C1-6)aminocarbonil-C1-6aIquilo; o R7 y R8 juntos representan -(CH2)n- donde n es 3, 4, o 6; o R7 y R8 junto con el átomo de nitrogeno al cual están unidos representan un anillo de 4, 5, 6 o 7 miembros que puede estar saturado o insaturado, donde, además del átomo de nitrogeno, el anillo puede contener un heteroátomo adicional seleccionado entre azufre, oxígeno y nitrogeno y/o puede condensarse a un anillo aromático o heteroaromático seleccionado entre fenilo, furilo, tienilo, pirrolilo, oxazolilo, isoxazolilo, tiazolilo, imidazolilo, pirazolilo, oxadiazolilo, tiadiazolilo, tetrazolilo, piridinilo, pirimidinilo, pirazinilo, piridazinilo, y donde el anillo puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, hidroxi, nitro, acilamino, trifluorometilo, alquilo C1-6, alcoxi C1-6, hidroxi-C1-6alquilo, alcoxi C1-6-aIquilo C1-6, COOH, CONH2, alcoxicarbonilo C1-6, alquilaminocarbonilo C1-6, arilaminocarbonilo, heteroarilaminocarbonilo, di-(alquil C1-6)aminocarbonilo, carboxi-C1-6alquilo, alcoxicarbonil C1-6-aIquilo C1-6, carbamoil-C1-6alquilo, ciclo-C3-12alquilo, arilo, heteroarilo, aril-C1-6alquilo, y heteroaril-C1-6alquilo; o R4 y R7 junto con los átomos de carbono y nitrogeno a los cuales están unidos representan un anillo de 5 o 6 miembros, donde el anillo puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre alquilo C1-6, arilo, heteroarilo, COOH, alcoxicarbonilo C1-6, y CONH2; donde el término ôariloö representa fenilo o naftilo, o fenilo sustituido con uno o más sustituyentes seleccionados entre halogeno, amino, hidroxi, nitro, ciano, COOH, CONH2, alquilaminocarbonilo C1-6, arilaminocarbonilo, heteroarilaminocarbonilo, hidroxi-C1-6alquilaminocarbonilo, di-(alquil C1-6)aminocarbonilo, trifluorometilo, aIquilo C1-6, heteroarilo, alcoxi C1-6, difluorometoxi, trifluorometoxi, ciclo-C3-12alcoxi, ariloxi, heteroariloxi, aril-C1-6alcoxi, heteroaril-C1-6alcoxi, amino-C1-6alquilo, hidroxi-C1-6alquilo, carboxi-C1-6alquilo, carbamoil-C1-6alquilo, ciano-C1-6alquilo, alcoxicarbonilamino C1-6-alquilo C1-6, hidroxi-C1-6alcoxi, carboxi-C1-6alcoxi, acil-C1-6alcoxi, alcoxicarbonilo C1-6, alquilamino C1-6, ciclo-C3-12alquilamino, arilamino, heteroarilamino, aril-C1-6alquilamino, heteroaril-C1-6alquilamino, hidroxi-C1-6alquilamino, carboxi-C1-6alquilamino, di-(alquil C1-6)amino, acilamino, di-(alquil C1-6)amino-C1-6alquilo, di-(alquil C1-6)amino-C1-6alquilamino-C1-6aIquilo, heterociclil-C1-6alquilo, alcoxicarbonil C1-6-alquilo C1-6, heterociclil-C1-6alquilo, ciano-C1-6alcoxi, heterociclil-C1-6aIcoxi, alquilamino C1-6-alcoxi C1-6, di-(alquil C1-6)amino-C1-6alcoxi, carboxi-C1-6alquilamino-C1-6alcoxi, alcoxicarbonil C1-6-alcoxi C1-6, heteroarilaminocarbonilC1-6alcoxi, alquilsulfonilamino C1-6, arilsulfonilamino, alquil C1-6-aminosulfonilo, di-(alquil C1-6)aminosulfonilo, arilaminosulfonilo, heteroarilaminosulfonilo, alquilaminocarbonil C1-6-alquilo C1-6, ciclo-C3-12alquilaminocarbonil-C1-6alquilo, arilaminocarbonil-C1-6alquilo, heteroarilaminocarbonil-C1-6alquilo, hidroxiC1-6alquilaminocarbonil-C1-6alquilo, carboxi-C1-6alquilaminocarbonil-C1-6alquilo, y di-(alquil C1-6)aminocarbonil-C1-6alquilo; y el término ôheteroariloö representa un anillo aromático de 5 o 6 miembros que comprende entre uno y cuatro heteroátomos seleccionados entre oxígeno, azufre y nitrogeno, o un grupo bicíclico que contiene un anillo de 5 o 6 miembros que comprende entre uno y cuatro heteroátomos seleccionados entre oxígeno, azufre y nitrogeno fusionado con un anillo benceno o con un anillo de 5 o 6 miembros que comprende entre uno y cuatro heteroátomos seleccionados entre oxígeno, azufre y nitrogeno, donde el heteroarilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, amino, hidroxi, nitro, ciano, COOH, CONH2, alquilaminocarbonilo C1-6, arilaminocarbonilo, heteroarilaminocarbonilo, hidroxi-C1-6alquilaminocarbonilo, di-(alquil C1-6)aminocarbonilo, trifluorometilo, alquilo C1-6, heteroarilo, alcoxi C1-6, difluorometoxi, trifluorometoxi, ciclo-C3-12alcoxi, ariloxi, heteroariloxi, aril-C1-6alcoxi, heteroaril-C1-6alcoxi, amino-C1-6alquilo, hidroxi-C1-6alquilo, carboxi-C1-6alquilo, carbamoil-C1-6alquilo, ciano-C1-6aIquilo, alcoxicarbonilamino C1-6-alquilo C1-6, hidroxi-C1-6alcoxi, carboxi-C1-6alcoxi, acil-C1-6alcoxi, alcoxicarbonilo C1-6, alquilamino C1-6, ciclo-C3-12alquilamino, arilamino, heteroarilamino, aril-C1-6alquilamino, heteroaril-C1-6alquilamino, hidroxi-C1-6alquilamino, carboxi-C1-6alquilamino, di-(alquil C1-6)amino, acilamino, di-(alquil C1-6)amino-C1-6alquilo, di-(alquil C1-6)amino-C1-6aIquilamino-C1-6alquilo, heterociclil-C1-6alquilo, alcoxicarbonil C1-6-alquilo C1-6, heterociclil-C1-6alquilo, ciano-C1-6alcoxi, heterociclil-C1-6alcoxi, alquilamino C1-6-alcoxi C1-6, di-(alquil C1-6)amino-C1-6alcoxi, carboxi-C1-6alquilamino-C1-6alcoxi, alcoxicarbonil C1-6-alcoxi C1-6, heteroarilaminocarbonil-C1-6alcoxi, alquilsulfonilamino C1-6, arilsulfonilamino, alquil C1-6-aminosulfonilo, di-(alquil C1-6)aminosulfonilo, arilaminosulfonilo, heteroarilaminosulfonilo, alquilaminocarbonil C1-6-alquilo C1-6, ciclo-C3-12alquilaminocarbonil-C1-6alquilo, arilaminocarbonil-C1-6aIquilo, heteroarilaminocarbonil-C1-6aIquilo, hidroxi-C1-6alquilaminocarbonil-C1-6alquilo, carboxi-C1-6alquilaminocarbonil-C1-6alquilo, y di-(alquil C1-6)aminocarbonil-C1-6alquilo; e isomeros opticos, polimorfos, análogos, derivados, prodrogas y sales de adicion ácida y básica e hidratos y solvatos farmacéuticamente aceptables del mismo. Reivindicacion 12: Una composicion farmacéutica, caracterizada porque comprende como principio activo un compuesto como se reivindica en cualquiera de las reivindicaciones precedentes, opcionalmente junto con uno o más excipientes farmacéuticamente aceptables. Reivindicacion 15: Uso de un compuesto como se reivindica en cualquiera de las reivindicaciones 1 a 11, caracterizado porque es para la fabricacion de un medicamento para el tratamiento o prevencion de una condicion que se selecciona de: dolor, incluyendo dolor agudo, dolor cronico, alodinia, hiperalgesia, dolor visceral, dolor fantasma, dolor postoperatorio, dolor neuropático, neuropatía periférica incluyendo, por ejemplo neuropatía periférica inducida por nocicepcion, inflamacion, isquemia, infeccion viral (HZV), lesion de nervi
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WO2013030358A1 (en) | 2011-08-31 | 2013-03-07 | Merz Pharma Gmbh & Co. Kgaa | Glycine b antagonists |
US9249085B2 (en) | 2011-09-16 | 2016-02-02 | Fovea Pharmaceuticals | Aniline derivatives, their preparation and their therapeutic application |
JP2015527403A (ja) * | 2012-09-11 | 2015-09-17 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Hivプロテアーゼ阻害剤 |
CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
CN106622375B (zh) * | 2016-12-17 | 2019-06-04 | 聊城大学 | 一种2,4-二羟基苯甲醛缩氨基酸镍催化剂、制备方法及应用 |
EP3366683A1 (en) | 2017-02-28 | 2018-08-29 | Acousia Therapeutics GmbH | Cyclic amides, acteamides and ureas useful as potassium channel openers |
WO2022087433A1 (en) * | 2020-10-23 | 2022-04-28 | Dana-Farber Cancer Institute, Inc. | Covalent inhibitors of creatine kinase (ck) and uses thereof for treating and preventing cancer |
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