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PE20060493A1 - COMPOUNDS DERIVED FROM BIPHENYL (DI OR TRI) CARBOXAMIDES AS SERINE / THREONINE KINASE P38 INHIBITORS - Google Patents

COMPOUNDS DERIVED FROM BIPHENYL (DI OR TRI) CARBOXAMIDES AS SERINE / THREONINE KINASE P38 INHIBITORS

Info

Publication number
PE20060493A1
PE20060493A1 PE2005001166A PE2005001166A PE20060493A1 PE 20060493 A1 PE20060493 A1 PE 20060493A1 PE 2005001166 A PE2005001166 A PE 2005001166A PE 2005001166 A PE2005001166 A PE 2005001166A PE 20060493 A1 PE20060493 A1 PE 20060493A1
Authority
PE
Peru
Prior art keywords
methyl
alkyl
cycloalkyl
serine
inhibitors
Prior art date
Application number
PE2005001166A
Other languages
Spanish (es)
Inventor
Jeffrey Charles Boehm
James Francis Callahan
Hongxing Yang
Zehong Wang
Original Assignee
Smithkline Beecham 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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20060493A1 publication Critical patent/PE20060493A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
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    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/63—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/67—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/68—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/69—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/78—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
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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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
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    • 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
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    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

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  • Ophthalmology & Optometry (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) EN DONDE R1 ES H, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON HALOGENO, CICLOALQUILO(C3-C7), ALCOXI(C1-C6), ENTRE OTROS; R2 ES H, ALQUILO(C1-C6) O -(CH2)P-CICLOALQUILO(C3-C7) OPCIONALMENTE SUSTITUIDO CON UNO O MAS GRUPOS ALQUILO(C1-C6) EN DONDE P ES 0 A 2; R3 ES HALOGENO O METILO; R4 ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C7), ENTRE OTROS; R8 ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C7), OPCIONALMENTE SUSTITUIDO; Y E X SE SELECCIONA INDEPENDIENTEMENTE ENTRE H, METILO Y HALOGENO; Z ES -(CH2)SCOOR16 O -(CH2)SCONR16R17, DONDE S ES 0 A 4, R16 Y R17 JUNTO CON NITROGENO FORMAN UN ANILLO DE 5 A 6 MIEMBROS OPCIONALMENTE SUSTITUIDO. SON COMPUESTOS PREFERIDOS: ACIDO 5'-[(CICLOPROPILAMINO)CARBONIL]-4-{[(2,2-DIMETILPROPIL)AMINO]-CARBONIL}-3'-FLUORO-2'-METIL-2-BIFENILCARBOXILICO, N2-[(1S)-1-CICLOHEXILETIL]-N3'-CICLOPROPIL-N4-(2,2-DIMETILPROPIL)-5'-FLUORO-6'-METIL-2,3',4-BIFENILTRICARBOXAMIDA, N3-CICLOPROPIL-N4'-(2,2-DIMETILPROPIL)-5-FLUORO-2'-[(4-HIDROXI-1-PIPERIDINIL)CARBONIL]-6-METIL-3,4'-BIFENILDICARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA SERINA/TREONINA QUINASA P38 SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES COMO ARTRITIS REUMATOIDE, ATEROSCLEROSISREFERS TO A COMPOUND OF FORMULA (I) WHERE R1 IS H, ALKYL (C1-C6) OPTIONALLY SUBSTITUTED WITH HALOGEN, CYCLOALKYL (C3-C7), ALCOXY (C1-C6), AMONG OTHERS; R2 IS H, ALKYL (C1-C6) OR - (CH2) P-CYCLOALKYL (C3-C7) OPTIONALLY SUBSTITUTED WITH ONE OR MORE ALKYL GROUPS (C1-C6) WHERE P IS 0 TO 2; R3 IS HALOGEN OR METHYL; R4 IS H, ALKYL (C1-C6), CYCLOALKYL (C3-C7), AMONG OTHERS; R8 IS H, ALKYL (C1-C6), CYCLOALKYL (C3-C7), OPTIONALLY SUBSTITUTED; Y E X IS SELECTED INDEPENDENTLY AMONG H, METHYL AND HALOGEN; Z IS - (CH2) SCOOR16 OR - (CH2) SCONR16R17, WHERE S IS 0 TO 4, R16 AND R17 TOGETHER WITH NITROGEN FORM AN OPTIONALLY REPLACED RING OF 5 TO 6 MEMBERS. THE PREFERRED COMPOUNDS ARE: 5 '- [(CYCLOPROPYLAMINO) CARBONYL ACID] -4 - {[(2,2-DIMETHYLPROPYL) AMINO] -CARBONYL} -3'-FLUORO-2'-METHYL-2-BIPHENYLCARBOXYL, N2 - [( 1S) -1-CYCLOHEXYLETHYL] -N3'-CYCLOPROPIL-N4- (2,2-DIMETHYLPROPYL) -5'-FLUORO-6'-METHYL-2,3 ', 4-BIPHENYLTRICARBOXAMIDE, N3-CYCLOPROPYL-N4' - ( 2,2-DIMETHYLPROPYL) -5-FLUORO-2 '- [(4-HYDROXY-1-PIPERIDINYL) CARBONYL] -6-METHYL-3,4'-BIPHENYLDICARBOXAMIDE, AMONG OTHERS. IT ALSO REFERS TO A PREPARATION PROCEDURE AND A PHARMACEUTICAL COMPOSITION. THESE COMPOUNDS ARE INHIBITORS OF SERINE / THREONINE KINASE P38, BEING USEFUL IN THE TREATMENT OF DISEASES SUCH AS RHEUMATOID ARTHRITIS, ATHEROSCLEROSIS

PE2005001166A 2004-10-05 2005-10-03 COMPOUNDS DERIVED FROM BIPHENYL (DI OR TRI) CARBOXAMIDES AS SERINE / THREONINE KINASE P38 INHIBITORS PE20060493A1 (en)

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