AR053366A1 - Derivados de aril - sulfonamidas como inhibidores especificos de caspasa-10, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de un medicamento para el tratamiento de la retinopatia diabetica. - Google Patents

Derivados de aril - sulfonamidas como inhibidores especificos de caspasa-10, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de un medicamento para el tratamiento de la retinopatia diabetica.

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Publication number
AR053366A1
AR053366A1 ARP060101575A ARP060101575A AR053366A1 AR 053366 A1 AR053366 A1 AR 053366A1 AR P060101575 A ARP060101575 A AR P060101575A AR P060101575 A ARP060101575 A AR P060101575A AR 053366 A1 AR053366 A1 AR 053366A1
Authority
AR
Argentina
Prior art keywords
group
formula
alkyl
atom
groups
Prior art date
Application number
ARP060101575A
Other languages
English (en)
Inventor
Claude Lardy
Marc Lecomte
Thierry Convard
Catherine Vidal
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR053366A1 publication Critical patent/AR053366A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/17—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • 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
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • 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
    • C07C323/46—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 at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms
    • C07C323/49—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 at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to sulfur atoms
    • 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
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Abstract

Compuestos de la formula general (1) para la preparacion de un medicamento para la prevencion o el tratamiento de retinopatía, en cuya formula (1) R1 representa un grupo de la formula -X-(Y)m, donde: -X- representa un grupo arilo, cicloalquilo, heteroarilo, alquilo o heterociclilo; cada uno de los grupos Y, iguales o diferentes, representa, de modo independiente, un átomo de halogeno o un grupo -alquilo, -O-alquilo, -CO-alquilo, -NO2, -perhaloalquilo, -S(O)p-alquilo o -perhaloalquilo, o dos grupos Y forman juntos un grupo arilo o heteroarilo condensado al nucleo fenilo al que están unidos; m representa un entero seleccionado de 0, 1, 2, 3, 4 y 5; R2 y R3 forman juntos un grupo cicloalquilo o heterociclilo opcionalmente sustituido con uno o varios grupos alquilo; R4 representa un grupo de la formula -Z-(alquil)n-Tp; donde -Z- representa -O- o un grupo -S(O)q- o, cuando n = p = 0, un átomo de halogeno o u grupo -OH; T representa un grupo cicloalquilo, heterociclilo o heteroarilo; n representa un entero seleccionado de 0 y 1; p representa un entero seleccionado de 0 y 1; i representa un entero mayor o igual a 2; R5 representa un átomo de H o un grupo alquilo, opcionalmente sustituido con uno o varios grupos cicloalquilo; cada uno de los grupos R6, iguales o diferentes, representa, de modo independiente, un grupo seleccionado de alquilo, O-alquilo, un átomo de halogeno y un grupo -CN, -NO2, -CO-alquilo, -CO2R, -NRR', -O-perhaloalquilo o, - perhaloalquilo; j representa un entero seleccionado de 0, 1, 2, 3 y 4; R y R', iguales o diferentes,. Representan, de modo independiente, un átomo de H o un grupo alquilo, q representa un entero seleccionado de 0, 1 y 2; y también las formas tautoméricas, enantioméricas, diastereoisoméricas y epiméricas, los ésteres y las sales farmacéuticamente aceptables. Y a su uso como inhibidores de caspasa-10, e especial para el tratamiento de retinopatía diabética, proveyendo además composiciones farmacéuticas que os comprenden. Reivindicacion 25: Proceso de preparacion de un compuesto de la formula (1), que comprende la etapa de preparacion de un compuesto de la correspondiente formula (2) en la que R23, R3, R6 y j son como se definieron en la formula (1) en la reivindicacion 15, i' representa 0 o i tal como se definio en la formula (1) en la reivindicacion 15 y R4' representa un átomo de H, o representa R4 tal como se definio en la formula (1) en la reivindicacion 15 o representa un grupo -Z-Gp en la que Gp representa un grupo lábil, o bien representa un grupo -CO2H, a partir de un compuesto de la formula (3) por accion de un compuesto de la formula (4) R1-SO2-Hal en la que R1 es tal como se definio en la formula (1) en la reivindicacion 15 y Hal representa un átomo de halogeno, con preferencia Cl, opcionalmente seguido, en el caso de que R5 sea distinto de H en la formula (2), por alquilacion del átomo de N.
ARP060101575A 2005-04-25 2006-04-21 Derivados de aril - sulfonamidas como inhibidores especificos de caspasa-10, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de un medicamento para el tratamiento de la retinopatia diabetica. AR053366A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR0504134A FR2884820B1 (fr) 2005-04-25 2005-04-25 Nouveaux inhibiteurs specifiques de la caspase-10

Publications (1)

Publication Number Publication Date
AR053366A1 true AR053366A1 (es) 2007-05-02

Family

ID=35431604

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060101575A AR053366A1 (es) 2005-04-25 2006-04-21 Derivados de aril - sulfonamidas como inhibidores especificos de caspasa-10, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de un medicamento para el tratamiento de la retinopatia diabetica.

Country Status (11)

Country Link
US (2) US8357721B2 (es)
EP (1) EP1881960B1 (es)
JP (1) JP5210153B2 (es)
AR (1) AR053366A1 (es)
AT (1) ATE502916T1 (es)
AU (1) AU2006239557B2 (es)
CA (1) CA2605748C (es)
DE (1) DE602006020855D1 (es)
ES (1) ES2362111T3 (es)
FR (1) FR2884820B1 (es)
WO (1) WO2006114190A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003061519A2 (en) * 2002-01-18 2003-07-31 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving the viability of photoreceptor cells
US9223209B2 (en) * 2010-02-19 2015-12-29 International Business Machines Corporation Sulfonamide-containing photoresist compositions and methods of use
US9223217B2 (en) * 2010-02-19 2015-12-29 International Business Machines Corporation Sulfonamide-containing topcoat and photoresist additive compositions and methods of use
WO2018234483A1 (en) * 2017-06-22 2018-12-27 Aaa Chemistry Aps TUNABLE PROBES FOR SELECTIVE PROTEIN MARKING AND ENZYMATIC INHIBITION

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2665440B1 (fr) * 1990-07-31 1994-02-04 Lipha Nouveaux cycloalkylsulfonamides substitues, procedes de preparation et medicaments les contenant.
EP0896533B1 (en) 1996-02-22 2003-09-10 Tularik, Inc. Pentafluorobenzenesulfonamides and analogs
FR2757509B1 (fr) * 1996-12-23 1999-03-26 Lipha Nouveaux derives de sulfonamides et sulfonylurees, leurs preparations et medicaments les contenant
US6379950B1 (en) * 1998-01-09 2002-04-30 Thomas Jefferson University Recombinant, active caspases and uses thereof
US20010006965A1 (en) * 1998-04-17 2001-07-05 Rifat Pamukcu Method for treating patients with diabetic retinopathy by administering substituted sulfonyl indenyl acetic acids and alcohols
FR2815541B1 (fr) * 2000-10-24 2008-02-29 Lipha Utilisation d'inhibiteurs de l'apoptose des pericytes pour le traitement et/ou la prevention de la retinopathie diabetique

Also Published As

Publication number Publication date
JP2008538774A (ja) 2008-11-06
AU2006239557A1 (en) 2006-11-02
DE602006020855D1 (de) 2011-05-05
CA2605748C (en) 2014-03-18
ES2362111T3 (es) 2011-06-28
CA2605748A1 (en) 2006-11-02
FR2884820A1 (fr) 2006-10-27
WO2006114190A1 (en) 2006-11-02
JP5210153B2 (ja) 2013-06-12
EP1881960B1 (en) 2011-03-23
ATE502916T1 (de) 2011-04-15
US8357721B2 (en) 2013-01-22
US20130090385A1 (en) 2013-04-11
FR2884820B1 (fr) 2007-07-27
US20080182906A1 (en) 2008-07-31
AU2006239557B2 (en) 2011-11-03
EP1881960A1 (en) 2008-01-30

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