AR042109A1 - Derivados de acido mandelico, procedimiento de preparacion, composicion farmaceutica que lo comprende, y, usos - Google Patents
Derivados de acido mandelico, procedimiento de preparacion, composicion farmaceutica que lo comprende, y, usosInfo
- Publication number
- AR042109A1 AR042109A1 ARP030104302A ARP030104302A AR042109A1 AR 042109 A1 AR042109 A1 AR 042109A1 AR P030104302 A ARP030104302 A AR P030104302A AR P030104302 A ARP030104302 A AR P030104302A AR 042109 A1 AR042109 A1 AR 042109A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkoxy
- carbonyl
- lower alkyl
- amino
- alkyl
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
- C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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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
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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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
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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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
- C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
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- 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
- C07D211/36—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
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/30—Oxygen atoms
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- 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
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
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- C07—ORGANIC CHEMISTRY
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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
- 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
- C07D213/56—Amides
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- 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
- C07D213/63—One oxygen atom
- C07D213/65—One oxygen atom attached in position 3 or 5
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- 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
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- 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
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
- C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
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- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
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- 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
- C07D295/145—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- 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
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- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Furan Compounds (AREA)
- Hydrogenated Pyridines (AREA)
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Abstract
La presente se refiere a derivados de ácido mandélico de la fórmula (1), así como a las sales fisiológicamente aceptables de los mismos. Estos compuestos inhiben la formación de los factores de coagulación Xa, IXa y trombina inducida por el factor VIIa y el factor hístico y pueden utilizarse como medicamentos. Reivindicación 1: Compuestos de la fórmula (1) en la que R1 es H, -OH, -NH2, (alcoxi inferior)-carbonilo, aril-(alcoxi inferior)-carbonilo, ariloxi-carbonilo, (alquilo inferior)-carbonilo, aril-carbonilo o (alcoxi inferior)-carbonilo que está sustituido por halógeno; R2, R3, y R4 con independencia entre sí se eligen entre H, halógeno, hidroxi, y alcoxi inferior; cuyo alcoxi inferior puede estar sustituido opcionalmente por hidroxi, carboxi o carbamoilo; R5 es alquilo inferior o cicloalquilo o, si X es O o NR12, R5 puede ser también H; R6 es H, alquilo inferior o flúor-alquilo inferior; Y es N o C-R11; R7, R8, R9, R10 y R11 con independencia entre sí se eligen entre H, hidroxi, halógeno, amino, (alquilo inferior)-amino, di-(alquilo inferior)-amino, (alquilo inferior)-carbonil-amino, NO2, flúor-alquilo inferior, alcoxi inferior, hidroxi-alcoxi inferior, flúor-alcoxi inferior, alquinilo inferior, hidroxi-alquinilo inferior, arilo, aril-alcoxi inferior, ariloxi, ariloxi-alcoxi inferior, heterociclilo, heterocicliloxi, (alcoxi inferior)-carbonil-alcoxi inferior, carbamoil-alcoxi inferior, carboxi-alcoxi inferior, cicloalquiloxi, heteroarilo, amino-alcoxi inferior, (alquilo inferior)-amino-alcoxi inferior y di-(alquilo inferior)-amino-alcoxi inferior; o R8 y R9 o R8 y R7 están unidos entre sí para formar un anillo junto con los átomos de C a los que están unidos y R8 y R9 juntos o R8 y R7 juntos son -O-CH2-O-, -O-CH2-CO-NH-, -O-CH2-CH2-CH2- o -CH=CH-CH=CH-, que pueden estar eventualmente sustituidos por alquilo inferior o alcoxi inferior y R10, R11 y R7 o R9 tienen respectivamente los significados definidos anteriormente; X es O, S, NR12 o SO2; R12 es H, alquilo inferior o (alquilo inferior)-carbonilo; y las sales farmacéuticamente aceptables de los mismos. Reivindicación 37: El uso de los compuestos según una cualquiera de las reivindicaciones 1-26 para la fabricación de medicamentos destinados al tratamiento terapéutico y/o profiláctico de trombosis arteriales y venosas, trombosis de venas profundas, embolia pulmonar, angina de pecho inestable, infarto cardíaco, apoplejía debida a fibrilación atrial, inflamación, arteriosclerosis y/o tumores.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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EP02026365 | 2002-11-25 |
Publications (1)
Publication Number | Publication Date |
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AR042109A1 true AR042109A1 (es) | 2005-06-08 |
Family
ID=32337999
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP030104302A AR042109A1 (es) | 2002-11-25 | 2003-11-21 | Derivados de acido mandelico, procedimiento de preparacion, composicion farmaceutica que lo comprende, y, usos |
Country Status (24)
Country | Link |
---|---|
US (1) | US7129238B2 (es) |
EP (1) | EP1567498B1 (es) |
JP (1) | JP4271657B2 (es) |
KR (1) | KR100705156B1 (es) |
CN (1) | CN1714079A (es) |
AR (1) | AR042109A1 (es) |
AT (1) | ATE384696T1 (es) |
AU (1) | AU2003292072B2 (es) |
BR (1) | BR0316508A (es) |
CA (1) | CA2505542A1 (es) |
CO (1) | CO5570663A2 (es) |
DE (1) | DE60318890T2 (es) |
ES (1) | ES2298583T3 (es) |
GT (1) | GT200300252A (es) |
MX (1) | MXPA05005446A (es) |
NO (1) | NO20052311L (es) |
PA (1) | PA8589201A1 (es) |
PE (1) | PE20040696A1 (es) |
PL (1) | PL377511A1 (es) |
RU (1) | RU2005120146A (es) |
TW (1) | TW200410921A (es) |
UY (1) | UY28090A1 (es) |
WO (1) | WO2004048335A2 (es) |
ZA (1) | ZA200503989B (es) |
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US7056932B2 (en) | 2003-12-19 | 2006-06-06 | Hoffman-La Roche Inc. | Heterocyclyl substituted 1-alkoxy acetic acid amides |
UA87854C2 (en) * | 2004-06-07 | 2009-08-25 | Мерк Энд Ко., Инк. | N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators |
RU2007112688A (ru) * | 2004-09-06 | 2008-10-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | Производные 4-аминометилбензамина и их применение в качестве ингибиторов фактора viia |
WO2007016358A1 (en) * | 2005-08-02 | 2007-02-08 | Merck & Co., Inc. | N-(pyridin-4-yl)-2-phenylbutanamides as androgen receptor modulators |
CN103641776A (zh) * | 2007-04-24 | 2014-03-19 | 日本曹达株式会社 | N-亚甲基取代甲胺多聚物的制造方法和三嗪衍生物 |
CN104370804A (zh) * | 2007-04-24 | 2015-02-25 | 日本曹达株式会社 | 取代甲胺化合物的制造方法 |
KR101682339B1 (ko) | 2007-04-24 | 2016-12-02 | 닛뽕소다 가부시키가이샤 | 치환 메틸아민 화합물의 제조방법 및 트리아진 유도체 |
US8217064B2 (en) * | 2007-12-20 | 2012-07-10 | Envivo Pharmaceuticals, Inc. | Tetrasubstituted benzenes |
WO2010022148A1 (en) * | 2008-08-19 | 2010-02-25 | The Trustees Of The University Of Pennsylvania | Methods for the preparation of irciniastatin and analogs thereof |
EP2272661A1 (en) * | 2009-07-10 | 2011-01-12 | Amcor Flexibles Transpac N.V. | Packaging material with integrated pressure relief valve |
US8343970B2 (en) | 2010-03-12 | 2013-01-01 | Omeros Corporation | PDE10 inhibitors and related compositions and methods |
GB201006042D0 (en) | 2010-04-12 | 2010-05-26 | Givaudan Sa | Improvements in or relating to organic compounds |
EP2578573A4 (en) | 2010-05-24 | 2014-08-06 | Toa Eiyo Ltd | CONDENSATE IMIDAZOLE DERIVATIVE |
CN103044176A (zh) * | 2012-12-12 | 2013-04-17 | 云南民族大学 | 一种氢气参与环醚开环制备卤代醇的高效方法 |
EP2931707A4 (en) * | 2012-12-13 | 2016-07-20 | Glaxosmithkline Llc | AMPLIFIER OF ZEST HOMOLOG 2 INHIBITORS |
NZ716462A (en) | 2014-04-28 | 2017-11-24 | Omeros Corp | Optically active pde10 inhibitor |
NZ716494A (en) | 2014-04-28 | 2017-07-28 | Omeros Corp | Processes and intermediates for the preparation of a pde10 inhibitor |
MY165587A (en) | 2014-07-29 | 2018-04-06 | Evonik Degussa Gmbh | Process for the epoxidation of an olefin |
EP3285760A4 (en) | 2015-04-24 | 2018-09-26 | Omeros Corporation | Pde10 inhibitors and related compositions and methods |
MY165609A (en) | 2015-04-28 | 2018-04-16 | Evonik Degussa Gmbh | Process for the epoxidation of propene |
JP2018535969A (ja) | 2015-11-04 | 2018-12-06 | オメロス コーポレーション | Pde10阻害剤の固体状態形態 |
JP6824269B2 (ja) | 2015-11-25 | 2021-02-03 | エボニック オペレーションズ ゲーエムベーハー | プロペンおよび過酸化水素から1,2−プロパンジオールを製造するための方法 |
CN108430983B (zh) | 2015-11-26 | 2022-02-22 | 赢创运营有限公司 | 用于丙烯的环氧化的方法和反应器 |
EP3380458B1 (en) | 2015-11-26 | 2019-07-24 | Evonik Degussa GmbH | Process for the epoxidation of propene |
TWI707847B (zh) | 2015-11-26 | 2020-10-21 | 德商贏創運營有限公司 | 丙烯之環氧化方法 |
EA033968B1 (ru) | 2015-11-26 | 2019-12-16 | Эвоник Дегусса Гмбх | Способ эпоксидирования олефина |
HUE050560T2 (hu) | 2016-01-19 | 2020-12-28 | Evonik Operations Gmbh | Eljárás olefin epoxidálására |
EA035906B1 (ru) | 2016-03-21 | 2020-08-28 | Эвоник Оперейшнс Гмбх | Способ эпоксидирования пропилена |
EP3246323A1 (en) | 2016-05-17 | 2017-11-22 | Evonik Degussa GmbH | Integrated process for making propene oxide from propane |
WO2018205244A1 (en) | 2017-05-12 | 2018-11-15 | Evonik Degussa Gmbh | Process for the epoxidation of propene |
EP3406603A1 (en) | 2017-05-22 | 2018-11-28 | Evonik Degussa GmbH | Process for the epoxidation of propene |
EP3438101A1 (en) | 2017-08-01 | 2019-02-06 | Evonik Degussa GmbH | Process for the epoxidation of propene |
AU2021290173A1 (en) * | 2020-06-10 | 2023-02-09 | Cyxone Ab | Rabeximod in the treatment of rheumatoid arthritis |
KR20240006545A (ko) | 2021-05-10 | 2024-01-15 | 에보닉 오퍼레이션스 게엠베하 | 프로펜 옥사이드를 제조하기 위한 통합 플랜트 및 통합 프로세스 |
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DE4128681A1 (de) * | 1991-08-29 | 1993-03-04 | Bayer Ag | Substituierte mandelsaeurederivate, verfahren zu ihrer herstellung sowie ihre verwendung in arzneimitteln |
US6060491A (en) * | 1997-06-19 | 2000-05-09 | Dupont Pharmaceuticals | 6-membered aromatics as factor Xa inhibitors |
PT921116E (pt) * | 1997-12-04 | 2003-11-28 | Hoffmann La Roche | Derivados de n-(4-carbamimido-fenil)-glicinamida |
EP1078917A4 (en) * | 1998-02-17 | 2002-11-06 | Ono Pharmaceutical Co | AMIDINO DERIVATIVES FOR USE AS ACTIVE INGREDIENTS AND MEDICINES CONTAINING THEM |
WO2000035858A1 (en) * | 1998-12-14 | 2000-06-22 | F. Hoffmann-La Roche Ag | Phenylglycine derivatives |
US6852761B2 (en) * | 2000-03-13 | 2005-02-08 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade |
US6548694B2 (en) * | 2000-05-23 | 2003-04-15 | Hoffman-La Roche Inc. | N-(4-carbamimidoyl-phenyl)-glycine derivatives |
DE10027024A1 (de) * | 2000-05-31 | 2001-12-06 | Merck Patent Gmbh | Carbaminsäureester |
DE10037146A1 (de) * | 2000-07-29 | 2002-02-07 | Merck Patent Gmbh | Acetamidderivate |
DE10040783A1 (de) * | 2000-08-21 | 2002-03-07 | Merck Patent Gmbh | AZA-Aminosäurederivate (Faktor X¶a¶-Inhibitoren 15) |
EP1193248A1 (en) * | 2000-09-30 | 2002-04-03 | Aventis Pharma Deutschland GmbH | Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation and their use |
DK1383731T3 (da) * | 2000-10-20 | 2009-12-07 | Biocryst Pharm Inc | Biarylforbindelser som serinproteaseinhibitorer |
AU2002231235A1 (en) * | 2000-11-07 | 2002-05-21 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
EP1364960A4 (en) * | 2001-02-02 | 2005-05-18 | Chugai Pharmaceutical Co Ltd | PEPTIDE DERIVATIVES |
GB0121337D0 (en) * | 2001-09-04 | 2001-10-24 | Astrazeneca Ab | Chemical compounds |
TW200410921A (en) | 2002-11-25 | 2004-07-01 | Hoffmann La Roche | Mandelic acid derivatives |
-
2003
- 2003-11-19 TW TW092132416A patent/TW200410921A/zh unknown
- 2003-11-20 PA PA20038589201A patent/PA8589201A1/es unknown
- 2003-11-21 CN CNA2003801035506A patent/CN1714079A/zh active Pending
- 2003-11-21 GT GT200300252A patent/GT200300252A/es unknown
- 2003-11-21 MX MXPA05005446A patent/MXPA05005446A/es active IP Right Grant
- 2003-11-21 AT AT03767602T patent/ATE384696T1/de not_active IP Right Cessation
- 2003-11-21 KR KR1020057009363A patent/KR100705156B1/ko not_active IP Right Cessation
- 2003-11-21 PL PL377511A patent/PL377511A1/pl not_active Application Discontinuation
- 2003-11-21 RU RU2005120146/04A patent/RU2005120146A/ru not_active Application Discontinuation
- 2003-11-21 EP EP03767602A patent/EP1567498B1/en not_active Expired - Lifetime
- 2003-11-21 BR BR0316508-6A patent/BR0316508A/pt not_active IP Right Cessation
- 2003-11-21 PE PE2003001183A patent/PE20040696A1/es not_active Application Discontinuation
- 2003-11-21 WO PCT/EP2003/013087 patent/WO2004048335A2/en active IP Right Grant
- 2003-11-21 JP JP2004554412A patent/JP4271657B2/ja not_active Expired - Fee Related
- 2003-11-21 ES ES03767602T patent/ES2298583T3/es not_active Expired - Lifetime
- 2003-11-21 AR ARP030104302A patent/AR042109A1/es not_active Application Discontinuation
- 2003-11-21 AU AU2003292072A patent/AU2003292072B2/en not_active Ceased
- 2003-11-21 CA CA002505542A patent/CA2505542A1/en not_active Abandoned
- 2003-11-21 US US10/720,790 patent/US7129238B2/en not_active Expired - Fee Related
- 2003-11-21 DE DE60318890T patent/DE60318890T2/de not_active Expired - Fee Related
- 2003-11-24 UY UY28090A patent/UY28090A1/es not_active Application Discontinuation
-
2005
- 2005-05-11 NO NO20052311A patent/NO20052311L/no unknown
- 2005-05-17 ZA ZA200503989A patent/ZA200503989B/en unknown
- 2005-05-23 CO CO05049707A patent/CO5570663A2/es not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
ATE384696T1 (de) | 2008-02-15 |
WO2004048335A3 (en) | 2004-08-19 |
JP2006515284A (ja) | 2006-05-25 |
EP1567498B1 (en) | 2008-01-23 |
GT200300252A (es) | 2004-06-28 |
NO20052311L (no) | 2005-06-16 |
US20040122057A1 (en) | 2004-06-24 |
US7129238B2 (en) | 2006-10-31 |
CA2505542A1 (en) | 2004-06-10 |
MXPA05005446A (es) | 2005-08-26 |
BR0316508A (pt) | 2005-10-04 |
ES2298583T3 (es) | 2008-05-16 |
EP1567498A2 (en) | 2005-08-31 |
ZA200503989B (en) | 2006-12-27 |
AU2003292072A1 (en) | 2004-06-18 |
PL377511A1 (pl) | 2006-02-06 |
PE20040696A1 (es) | 2004-10-08 |
UY28090A1 (es) | 2004-05-31 |
WO2004048335A2 (en) | 2004-06-10 |
PA8589201A1 (es) | 2004-07-26 |
CN1714079A (zh) | 2005-12-28 |
TW200410921A (en) | 2004-07-01 |
KR20050086774A (ko) | 2005-08-30 |
AU2003292072B2 (en) | 2006-12-07 |
DE60318890D1 (de) | 2008-03-13 |
DE60318890T2 (de) | 2009-01-15 |
CO5570663A2 (es) | 2005-10-31 |
KR100705156B1 (ko) | 2007-04-09 |
RU2005120146A (ru) | 2006-05-10 |
JP4271657B2 (ja) | 2009-06-03 |
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