AR091144A1 - Compuestos inhibidores de la actividad de la catecol o-metiltransferasa - Google Patents

Compuestos inhibidores de la actividad de la catecol o-metiltransferasa

Info

Publication number
AR091144A1
AR091144A1 ARP130101802A AR091144A1 AR 091144 A1 AR091144 A1 AR 091144A1 AR P130101802 A ARP130101802 A AR P130101802A AR 091144 A1 AR091144 A1 AR 091144A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
aryl
substituted
independently
Prior art date
Application number
Other languages
English (en)
Inventor
Vaismaa Matti
Messinger Josef
Pystynen Jarmo
Din Belle David
Kauppala Mika
Luiro Anne
Pajunen Taina
Tiainen Eija
Ahlmark Marko
Original Assignee
Orion Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Orion Corp filed Critical Orion Corp
Publication of AR091144A1 publication Critical patent/AR091144A1/es

Links

Classifications

    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A61K31/198—Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/382—Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07C255/53—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07C255/57—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07C255/59—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 the carbon skeleton being further substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66—Methanesulfonates
    • 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
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/46—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/24—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/29—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/57—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D213/60—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
    • C07D213/62—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/34—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/70—Sulfur atoms
    • C07D277/74—Sulfur atoms substituted by carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/80—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D309/06—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/20—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hydrogen atoms and substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D309/22—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/28—Halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2

Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), donde R¹ es alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, cicloalquenilo C₄₋₁₀, arilo, (R²)₂C=C-, halógeno, hidroxi, alcoxi C₁₋₆, alquil C₁₋₆-S-, cicloalqueniloxi C₄₋₁₀, cicloalquenil C₄₋₁₀-S-, ariloxi, aril-S-, heteroariloxi, heteroaril-S-, (R³)₂N-, (R⁴)₂C=N-, heterociclilo, heteroarilo, arilalquilo C₁₋₆, (1-amino-1-carboximetil)-alquilo C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, alcoxi C₁₋₆alquilo C₁₋₆, alquil C₁₋₆-S-alquilo C₁₋₆, (R³)₂N-alquilo C₁₋₆, heterociclil-alquilo C₁₋₆, carboxi-alquenilo C₂₋₆, cicloalquil C₃₋₇alquenilo C₂₋₆, aril-alquenilo C₂₋₆, alcoxi C₁₋₆alquenilo C₂₋₆, heterociclil-alquenilo C₂₋₆, heteroaril-alquenilo C₂₋₆, carboxi-alquinilo C₂₋₆, cicloalquil C₃₋₇-alquinilo C₂₋₆, aril-alquinilo C₂₋₆, alcoxi C₁₋₆alquinilo C₂₋₆, heterociclil-alquinilo C₂₋₆, heteroaril-alquinilo C₂₋₆, haloalcoxi C₁₋₆, hidroxi-alcoxi C₁₋₆, alcoxi C₁₋₆alcoxi C₁₋₆, alquil C₁₋₆-(C=O)-O-, R⁵-(S=O)-, R⁵-(O=S=O)-, hidroxi-alcoxi C₁₋₆alquilo C₁₋₆, alcoxi C₁₋₆-(C=O)-alquenilo C₂₋₆ o alquil C₁₋₆-(C=O)-O-alquilo C₁₋₆, donde dicho cicloalquenilo C₄₋₁₀, arilo, heterociclilo, heteroarilo o cicloalquilo C₃₋₇ como tal o como parte de otro grupo no está sustituido o está sustituido con 1, 2 ó 3 sustituyente(s) R⁶; R² es, en forma independiente en cada caso, carboxi o arilo, donde dicho arilo, en forma independiente en cada caso, no está sustituido o está sustituido con 1, 2 ó 3 sustituyente(s) R⁶; R³ es, en forma independiente en cada caso, H, alquilo C₁₋₆, cicloalquilo C₃₋₇, arilo, cicloalquil C₃₋₇alquilo C₁₋₆, hidroxialquilo C₁₋₆ o alcoxi C₁₋₆alquilo C₁₋₆, donde dicho cicloalquilo C₃₋₇ o arilo como tal o como parte de otro grupo, en forma independiente en cada caso, no está sustituido o está sustituido con 1 sustituyente que es alquilo C₁₋₆, halógeno, hidroxi, alcoxi C₁₋₆ o hidroxialquilo C₁₋₆; R⁴ es, en forma independiente en cada caso, H o arilo, donde dicho arilo, en forma independiente en cada caso, no está sustituido o está sustituido con 1 sustituyente que es alquilo C₁₋₆, halógeno o alcoxi C₁₋₆; R⁵ es alquilo C₁₋₆, arilo, hidroxi o alcoxi C₁₋₆, donde dicho arilo no está sustituido o está sustituido con 1, 2 ó 3 sustituyente(s) R⁶; R⁶ es, en forma independiente en cada caso, alquilo C₁₋₆, alquenilo C₂₋₆, carboxi, ciano, arilo, halógeno, hidroxi, alcoxi C₁₋₆, alquil C₁₋₆-S-, cicloalqueniloxi C₄₋₁₀, cicloalquenil C₄₋₁₀-S-, ariloxi, aril-S-, heteroariloxi, heteroaril-S-, (R⁷)₂N-, heteroarilo, carboxialquilo C₁₋₆, arilalquilo C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, alcoxi C₁₋₆alquilo C₁₋₆, heterociclilalquilo C₁₋₆, alquil C₁₋₆-(C=O)-, alcoxi C₁₋₆-(C=O)-, heterociclil-(C=O)-, (R⁷)₂N-(C=O)-, haloalcoxi C₁₋₆, R⁸-(S=O)-, R⁸-(O=S=O)-, alcoxi C₁₋₆-(C=O)-alquilo C₁₋₆, (R⁷)₂N-(C=O)-alquilo C₁₋₆ o alcoxi C₁₋₆alcoxi C₁₋₆-(C=O)-, donde dicho arilo, heteroarilo o heterociclilo como tal o como parte de otro grupo, en forma independiente en cada caso, no está sustituido o está sustituido con 1 sustituyente que es alquilo C₁₋₆; o R⁶ y R⁶ unidos al mismo átomo de carbono del anillo forman, junto con el átomo de carbono del anillo al cual están unidos, un grupo -(C=O)-; R⁷ es, en forma independiente en cada caso, H, alquilo C₁₋₆, cicloalquilo C₃₋₇ o carboxialquilo C₁₋₆, donde dicho cicloalquilo C₃₋₇, en forma independiente en cada caso, no está sustituido o está sustituido con 1 sustituyente que es alquilo C₁₋₆; R⁸ es, en forma independiente en cada caso, alquilo C₁₋₆, hidroxi, alcoxi C₁₋₆ o (R⁹)₂N-; R⁹ es, en forma independiente en cada caso, alquilo C₁₋₆; o una sal o éster farmacéuticamente aceptable de los mismos.
ARP130101802 2012-05-24 2013-05-23 Compuestos inhibidores de la actividad de la catecol o-metiltransferasa AR091144A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261651217P 2012-05-24 2012-05-24
US201361777162P 2013-03-12 2013-03-12

Publications (1)

Publication Number Publication Date
AR091144A1 true AR091144A1 (es) 2015-01-14

Family

ID=48669995

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130101802 AR091144A1 (es) 2012-05-24 2013-05-23 Compuestos inhibidores de la actividad de la catecol o-metiltransferasa

Country Status (35)

Country Link
US (6) US9458128B2 (es)
EP (1) EP2855426B1 (es)
JP (1) JP6181747B2 (es)
KR (1) KR102100612B1 (es)
CN (1) CN104334525B (es)
AR (1) AR091144A1 (es)
AU (1) AU2013265119B2 (es)
BR (1) BR112014029139B1 (es)
CA (1) CA2871801C (es)
CL (1) CL2014003191A1 (es)
CO (1) CO7151502A2 (es)
CY (1) CY1118740T1 (es)
DK (1) DK2855426T3 (es)
EA (1) EA028466B1 (es)
ES (1) ES2613692T3 (es)
HK (1) HK1208859A1 (es)
HR (1) HRP20170487T1 (es)
HU (1) HUE031366T2 (es)
IL (1) IL235396A (es)
LT (1) LT2855426T (es)
MD (1) MD4556C1 (es)
MX (1) MX357896B (es)
MY (1) MY168539A (es)
NZ (1) NZ701982A (es)
PE (1) PE20150024A1 (es)
PH (1) PH12014502588B1 (es)
PL (1) PL2855426T3 (es)
PT (1) PT2855426T (es)
RS (1) RS55840B1 (es)
SG (1) SG11201407037UA (es)
SI (1) SI2855426T1 (es)
TN (1) TN2014000474A1 (es)
TW (1) TWI638802B (es)
WO (1) WO2013175053A1 (es)
ZA (1) ZA201408215B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6258928B2 (ja) 2012-06-13 2018-01-10 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規ジアザスピロシクロアルカンおよびアザスピロシクロアルカン
PT2900669T (pt) 2012-09-25 2019-10-29 Hoffmann La Roche Derivados de hexahidropirrolo[3,4−c]pirrol e compostos relacionados enquanto inibidores da autotaxina (atx) e enquanto inibidores da produção de ácido lisofosfatídico (lpa) para o tratamento de, por exemplo, doenças renais
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
WO2015078803A1 (en) 2013-11-26 2015-06-04 F. Hoffmann-La Roche Ag NEW OCTAHYDRO-CYCLOBUTA [1,2-c;3,4-c']DIPYRROL-2-YL
CN106029667B (zh) 2014-03-26 2019-08-23 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的稠合[1,4]二氮杂*化合物
SI3122750T1 (sl) 2014-03-26 2019-12-31 F. Hoffmann-La Roche Ag Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA)
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
UA123362C2 (uk) 2015-09-04 2021-03-24 Ф. Хоффманн-Ля Рош Аг Феноксиметильні похідні
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ａｔｘ阻害剤としての二環式化合物
CN107922415B (zh) 2015-09-24 2022-04-15 豪夫迈·罗氏有限公司 新的作为双重atx/ca抑制剂的二环化合物
MX2017015034A (es) 2015-09-24 2018-04-13 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
CA3053329A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag Heterocyclic compounds useful as dual atx/ca inhibitors
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
WO2019097120A1 (en) 2017-11-16 2019-05-23 Orion Corporation New use and pharmaceutical dosage forms
JP2021532133A (ja) * 2018-07-25 2021-11-25 オリオン コーポレーション ４，５−ジヒドロキシ−２−（４−メチルベンジル）イソフタロニトリル溶媒和物およびその結晶形
US20220002232A1 (en) * 2018-11-09 2022-01-06 Orion Corporation Process for the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile
EP3966870B1 (en) * 2019-05-09 2024-04-03 Merck Patent GmbH Aromatic compounds
CN110632211A (zh) * 2019-10-18 2019-12-31 上海明捷医药科技有限公司 一种测定药物中2-巯基苯并噻唑迁移量的方法
CN112645971B (zh) * 2021-01-20 2021-12-24 中国科学院兰州化学物理研究所 一种烷基卤代物直接制备烷基硼酸酯类化合物的方法

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5035393A (es) * 1973-08-01 1975-04-04
US5236952A (en) 1986-03-11 1993-08-17 Hoffmann-La Roche Inc. Catechol derivatives
ZA871564B (en) * 1986-03-11 1987-10-28 Hoffmann La Roche 3,5-disubstituted pyrocatechole derivatives
DK175069B1 (da) * 1986-03-11 2004-05-24 Hoffmann La Roche Pyrocatecholderivater
YU213587A (en) * 1986-11-28 1989-06-30 Orion Yhtymae Oy Process for obtaining new pharmacologic active cateholic derivatives
US5283352A (en) * 1986-11-28 1994-02-01 Orion-Yhtyma Oy Pharmacologically active compounds, methods for the preparation thereof and compositions containing the same
DE4240321A1 (de) 1992-12-01 1994-06-09 Basf Ag Verfahren zur Herstellung von aromatischen Vinylverbindungen
DE4421730C1 (de) 1994-06-22 1995-11-23 Hoechst Ag Verfahren zur Herstellung von aromatischen Olefinen unter Katalyse von Palladacyclen
GB9510481D0 (en) * 1995-05-24 1995-07-19 Orion Yhtymae Oy New catechol derivatives
DE19647582A1 (de) 1996-11-18 1998-05-20 Hoechst Ag Verfahren zur Herstellung von aromatischen Olefinen mittels Katalyse durch Palladaphosphacyclobutane
GB9626472D0 (en) * 1996-12-20 1997-02-05 Aperia Anita C New use of comt inhibitors
DE19825454A1 (de) 1998-06-06 1999-12-16 Aventis Res & Tech Gmbh & Co Verfahren zur Herstellung von aromatischen Olefinen unter Katalyse von Palladiumkatalysatoren mit Phosphitliganden
US6215035B1 (en) 1998-09-25 2001-04-10 Council Of Scientific And Industrial Research Process for the preparation of aralkylated aromatic compounds using heterogeneous catalyst
GB2344819A (en) 1998-12-18 2000-06-21 Portela & Ca Sa 2-Phenyl-1-(3,4-dihydroxy-5-nitrophenyl)-1-ethanones
FI20000635A0 (fi) * 2000-03-17 2000-03-17 Orion Yhtymae Oyj COMT-inhibiittoreiden käyttö analgeettina
GB2363792A (en) 2000-06-21 2002-01-09 Portela & Ca Sa Nitrocatechols
GB0015228D0 (en) 2000-06-21 2000-08-16 Portela & Ca Sa Substituted nitrated catechols, their use in the treatment of some central and peripheral nervous system disorders
FI20001593A (fi) 2000-07-03 2002-01-04 Orion Yhtymo Oyj Comt-entsyymiõ inhiboivaa aktiivisuutta omaavia kumariinijohdannaisia
FI20002044A0 (fi) 2000-09-15 2000-09-15 Orion Yhtymae Oyj Comt-entsyymiä estäviä naftaleenijohdannaisia
US6548722B1 (en) 2000-10-10 2003-04-15 Council Of Scientific And Industrial Research Process for the preparation of substituted aromatic compound employing friedel-crafts reaction using a reusable basic anionic clay catalyst
JP2005516967A (ja) 2002-01-18 2005-06-09 ザ ジェネティクス カンパニー インコーポレーティッド β−セクレターゼインヒビター
US20070142399A1 (en) 2003-06-19 2007-06-21 Psychiatric Genomics, Inc. Dual function drugs and uses thereof
WO2005058228A2 (en) 2003-12-19 2005-06-30 F. Hoffmann-La Roche Ag Comt inhibitors
EP1812070B1 (en) * 2004-11-10 2013-10-02 Orion Corporation Treatment of restless legs syndrome
MY148644A (en) 2005-07-18 2013-05-15 Orion Corp New pharmaceutical compounds
DK1907382T3 (en) 2005-07-26 2015-08-31 Bial Portela & Ca Sa Nitrocatecholderivater comt inhibitors as
CA2621261C (en) * 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
US20070219192A1 (en) 2005-11-02 2007-09-20 Xiangping Qian Certain chemical entities, compositions, and methods
WO2007063789A1 (ja) 2005-11-29 2007-06-07 Kissei Pharmaceutical Co., Ltd. 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
US20100048713A1 (en) 2006-01-06 2010-02-25 Aarhus Universitet Compounds acting on the serotonin transporter
EP1845097A1 (en) 2006-04-10 2007-10-17 Portela & Ca., S.A. Oxadiazole derivatives as COMT inhibitors
WO2008024963A1 (en) 2006-08-24 2008-02-28 Serenex, Inc. Benzene, pyridine, and pyridazine derivatives
JP2010510177A (ja) 2006-11-17 2010-04-02 クイーンズ ユニバーシティ アット キングストン タンパク質フォールディング障害を治療するための化合物および方法
JP2008308494A (ja) 2007-05-17 2008-12-25 Kissei Pharmaceut Co Ltd 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
JP2008308493A (ja) 2007-05-17 2008-12-25 Kissei Pharmaceut Co Ltd 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
JP2008308495A (ja) 2007-05-17 2008-12-25 Kissei Pharmaceut Co Ltd 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
TWI415607B (zh) 2007-12-25 2013-11-21 Kissei Pharmaceutical 新穎兒茶酚衍生物、含有其之醫藥組成物及該等之用途
JP5369000B2 (ja) 2007-12-25 2013-12-18 キッセイ薬品工業株式会社 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
ES2402562T3 (es) 2008-07-04 2013-05-06 Kissei Pharmaceutical Co., Ltd. Derivado de catecol y su uso
WO2010011318A2 (en) 2008-07-23 2010-01-28 Massachusetts Institute Of Technology Activatiqn of histone deacetylase 1 (hdac1) protects against dna damage and increases neuronal survival
US10532034B2 (en) 2009-03-25 2020-01-14 Cornell University Inhibition of glutaminase C
JP5707063B2 (ja) 2009-06-18 2015-04-22 キッセイ薬品工業株式会社 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
CN101643465A (zh) 2009-08-14 2010-02-10 东华大学 一种comt抑制剂5,6,7,3＇,4＇-五甲氧基异黄酮的制备方法
MX2012010187A (es) 2010-03-04 2012-10-03 Merck Sharp & Dohme Inhibidores de catecol o-metil transferasa y su uso en el tratamiento de transtornos psicoticos.
WO2011109261A1 (en) 2010-03-04 2011-09-09 Merck Sharp & Dohme Corp. Inhibitors of catechol o-methyl transferase and their use in the treatment of psychotic disorders
ES2662332T3 (es) 2010-03-04 2018-04-06 Merck Sharp & Dohme Corp. Inhibidores de la catecol-O-metil-transferasa y su uso en el tratamiento de trastornos psicóticos
JP5883590B2 (ja) 2010-08-06 2016-03-15 キッセイ薬品工業株式会社 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
JP5883591B2 (ja) 2010-08-06 2016-03-15 キッセイ薬品工業株式会社 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
EP2655334B1 (en) 2010-12-22 2018-10-03 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
GB201107176D0 (en) 2011-04-28 2011-06-15 Cxr Biosciences Ltd Pyrrolnitrin derivatives
CN102755312A (zh) 2012-07-16 2012-10-31 中国科学院大连化学物理研究所 具有黄酮骨架结构的化合物作为帕金森症治疗药物的应用

Also Published As

Publication number Publication date
EA028466B1 (ru) 2017-11-30
US20200352898A1 (en) 2020-11-12
RS55840B1 (sr) 2017-08-31
HUE031366T2 (en) 2017-07-28
KR102100612B1 (ko) 2020-04-16
JP6181747B2 (ja) 2017-08-16
CY1118740T1 (el) 2017-07-12
JP2015522547A (ja) 2015-08-06
PT2855426T (pt) 2017-03-06
TW201408629A (zh) 2014-03-01
CN104334525A (zh) 2015-02-04
DK2855426T3 (en) 2017-03-06
BR112014029139A2 (pt) 2017-06-27
TWI638802B (zh) 2018-10-21
US20150218124A1 (en) 2015-08-06
ZA201408215B (en) 2015-12-23
WO2013175053A1 (en) 2013-11-28
US20200009103A1 (en) 2020-01-09
KR20150013198A (ko) 2015-02-04
MY168539A (en) 2018-11-12
AU2013265119B2 (en) 2017-03-30
CA2871801C (en) 2020-07-21
MD4556B1 (ro) 2018-03-31
CO7151502A2 (es) 2014-12-29
PL2855426T3 (pl) 2017-07-31
NZ701982A (en) 2017-10-27
EP2855426A1 (en) 2015-04-08
MD20140124A2 (ro) 2015-03-31
CA2871801A1 (en) 2013-11-28
SG11201407037UA (en) 2014-12-30
AU2013265119A1 (en) 2014-11-20
BR112014029139A8 (pt) 2021-06-08
BR112014029139B1 (pt) 2022-07-19
IL235396A (en) 2017-10-31
PH12014502588A1 (en) 2015-02-09
HRP20170487T1 (hr) 2017-06-02
US20190029990A1 (en) 2019-01-31
TN2014000474A1 (en) 2016-03-30
MX357896B (es) 2018-07-27
US20170165219A1 (en) 2017-06-15
EA201492210A1 (ru) 2015-05-29
PE20150024A1 (es) 2015-01-25
CL2014003191A1 (es) 2015-01-23
MX2014014311A (es) 2015-02-12
MD4556C1 (ro) 2018-10-31
US20220047540A1 (en) 2022-02-17
LT2855426T (lt) 2017-03-10
ES2613692T3 (es) 2017-05-25
HK1208859A1 (en) 2016-03-18
SI2855426T1 (sl) 2017-05-31
US9458128B2 (en) 2016-10-04
PH12014502588B1 (en) 2015-02-09
CN104334525B (zh) 2017-05-10
EP2855426B1 (en) 2017-01-04

Similar Documents

Publication Publication Date Title
AR091144A1 (es) Compuestos inhibidores de la actividad de la catecol o-metiltransferasa
CR20170066A (es) Compuestos aminopirimidinilo como inhibidires de jak
CY1120635T1 (el) Βενζαμιδια αμινοετεροαρυλιου ως αναστολεις κινασης
PH12017502171B1 (en) PYRIDO[3,4-d]PYRIMIDINE DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
CO7180199A2 (es) Imidazotriazincarbonitrilos útiles como inhibidores de cinasa
BR112017019286A2 (pt) composto de fórmula (i) ou um sal farmaceuticamente aceitável deste
PE20151423A1 (es) Derivados tetrahidropiranilo inhibidores del hcv
MD20140136A2 (ro) Inhibitori ai virusului hepatic C
UY33488A (es) Derivados de imidazopiridina, su procedimiento y preparacion y su aplicacion en terapeutica
AR089781A1 (es) Fluorometil-5,6-dihidro-4h-[1,3]oxazinas
AR088829A1 (es) DERIVADOS DE CICLOHEXILAMINA QUE TIENEN ACTIVIDAD COMO AGONISTAS ADRENERGICOS b2 Y COMO ANTAGONISTAS MUSCARINICOS M3
AR097279A1 (es) Derivados de benzimidazolil-metil urea como agonistas del receptor de alx
CR20150378A (es) Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas
AR094812A1 (es) Derivado de piridina monocíclico como inhibidor del fgfr
EA201591486A1 (ru) Соединения имидазопиридина
ES2626801T3 (es) Compuestos de triazolopiridina como inhibidores de pde10a
AR095359A1 (es) Compuestos heteroaromáticos y su uso como ligandos d1 de dopamina
AR103742A1 (es) Derivados de trifluorometilpropanamida
CU20170007A7 (es) Compuestos de imidazopiridazina
EA201492255A1 (ru) Феноксиэтилпиперидиновые соединения
EA201590621A1 (ru) Ингибиторы аггреканазы
AR100439A1 (es) Derivados de carboxamida
AR100776A1 (es) Compuestos herbicidas
MX2015013224A (es) Inhibidores macrociclicos y biciclicos del virus de la hepatitis c.
MX2018002018A (es) Derivado de urea y uso del mismo.

Legal Events

Date Code Title Description
FC Refusal