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AR035478A1 - AMIDA-HYDROXAMIC ACID, ACETYLLENE, BETA-SULPHONAMIDE AND PHOSPHINIC ACID AS INHIBITORS OF TACE, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PHARMACEUTICAL COMPOSITION CONTAINING THEM - Google Patents

AMIDA-HYDROXAMIC ACID, ACETYLLENE, BETA-SULPHONAMIDE AND PHOSPHINIC ACID AS INHIBITORS OF TACE, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PHARMACEUTICAL COMPOSITION CONTAINING THEM

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Publication number
AR035478A1
AR035478A1 ARP000100325A ARP000100325A AR035478A1 AR 035478 A1 AR035478 A1 AR 035478A1 AR P000100325 A ARP000100325 A AR P000100325A AR P000100325 A ARP000100325 A AR P000100325A AR 035478 A1 AR035478 A1 AR 035478A1
Authority
AR
Argentina
Prior art keywords
heteroatoms selected
membered
phenyl
alkyl
cycloalkyl
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Application number
ARP000100325A
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Spanish (es)
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Wyeth Corp
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Publication of AR035478A1 publication Critical patent/AR035478A1/en

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    • C07C309/78—Halides of sulfonic acids
    • C07C309/86—Halides of sulfonic acids having halosulfonyl groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/87—Halides of sulfonic acids having halosulfonyl groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing singly-bound oxygen atoms bound to the carbon skeleton
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    • C07—ORGANIC CHEMISTRY
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/50—Organo-phosphines
    • C07F9/53—Organo-phosphine oxides; Organo-phosphine thioxides
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/41—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing singly-bound oxygen atoms bound to the carbon skeleton
    • C07C309/42—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing singly-bound oxygen atoms bound to the carbon skeleton having the sulfo groups bound to carbon atoms of non-condensed six-membered aromatic rings
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    • 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
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    • C07C2601/14—The ring being saturated

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Abstract

Acidos de hidroxamida, caracterizada porque comprenden la fórmula (1) en la cual la parte C(=O) NHOH y la parte -NR5- están unidas a carbonos adyacentes; donde: X es SO2 o -P(O)R10; Y es un anillo de heteroarilo con 5-10 miembros, que tiene entre 1-3 heteroátomos seleccionados entre: N, NR9, S y O, fenilo o naftilo; con la condición de que X y Z pueden no estar ligados a átomos adyacentes de Y; Z es O, NH, CH2 o S; R5 es hidrógeno o alquilo C1-6; R6 y R7 cada uno, de un modo, independiente, son hidrógeno o metilo; R8 es hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, un heteroarilo de 5-7 miembros con 1-3 heteroátomos seleccionados entre; N, NR9, S y O, un heterocicloalquilo de 5 a 7 miembros que tiene 1 o 2 heteroátomos seleccionados entre N, NR9, S y O, o fenilo; Rg es hidrógeno, alquilo C1-6, cicloalquilo C3-6, o fenilo; R10 es alquilo C1-6, cicloalquilo C3-6, fenilo, o heteroarilo de 5 a 7 miembros, con 1-3 heteroátomos seleccionados entre N, NR9, S y O; R11 y R12 son, de un modo independiente, hidrógeno, alquilo C1-6, cicloalquilo C3-6, un heteroarilo de 5 a 7 miembros que tiene 1-3 heteroátomos seleccionados entre N, NR9, S y O, un heterocicloalquilo de 5 a 7 miembros con 1 o 2 heteroátomos seleccionados entre N, NR9, S y O, o fenilo y el enlace doble opcional que está representado por la línea de puntos está presente; o R11 y R12, junto con los carbonos a los que están unidos, forman un anillo de alquilo mono- o bicíclico, de 5 a 10 miembros saturado o insaturado, opcionalmente fusionado a un anillo de cicloalquilo de 5 a 7 miembros saturado o insaturado, un heteroarilo de 5 a 7 miembros con 1-3 heteroátomos seleccionados entre N, NR9, S y O, un heterocicloalquilo de 5 a 7 miembros con 1 o 2 heteroátomos seleccionados entre N, NR9, S y O, anillos de fenilo o naftilo; o R11 y R12, junto con los carbonos a Los que están unidos, forman un heterocicloalquilo mono- o bicíclico, de 5 a 10 miembros saturado o insaturado, con 1-2 heteroátomos seleccionados entre N, NR9, S y O, opcionalmente fusionados a un heteroarilo de 5 a 7 miembros mono- o bicíclico con 5 a 7 miembros, de 1 a 3 heteroátomos seleccionados entre N, NR9, S y O, un anillo de cicloalquilo de 5 a 7 miembros, saturado o insaturado o un anillo de fenilo o naftilo; la línea de puntos representa un enlace doble opcional; y n = 0-2, o una sal farmacéuticamente aceptable de los mismos.Hydroxamide acids, characterized in that they comprise formula (1) in which part C (= O) NHOH and part -NR5- are attached to adjacent carbons; where: X is SO2 or -P (O) R10; Y is a 5-10 membered heteroaryl ring, which has between 1-3 heteroatoms selected from: N, NR9, S and O, phenyl or naphthyl; with the proviso that X and Z may not be linked to adjacent atoms of Y; Z is O, NH, CH2 or S; R5 is hydrogen or C1-6 alkyl; R6 and R7 each, independently, are hydrogen or methyl; R 8 is hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, a 5-7 membered heteroaryl with 1-3 heteroatoms selected from; N, NR9, S and O, a 5- to 7-membered heterocycloalkyl having 1 or 2 heteroatoms selected from N, NR9, S and O, or phenyl; Rg is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, or phenyl; R10 is C1-6 alkyl, C3-6 cycloalkyl, phenyl, or 5-7 membered heteroaryl, with 1-3 heteroatoms selected from N, NR9, S and O; R11 and R12 are, independently, hydrogen, C1-6 alkyl, C3-6 cycloalkyl, a 5- to 7-membered heteroaryl having 1-3 heteroatoms selected from N, NR9, S and O, a 5 to heterocycloalkyl 7 members with 1 or 2 heteroatoms selected from N, NR9, S and O, or phenyl and the optional double bond that is represented by the dotted line is present; or R11 and R12, together with the carbons to which they are attached, form a saturated or unsaturated 5 to 10 membered mono- or bicyclic alkyl ring, optionally fused to a saturated or unsaturated 5 to 7 membered cycloalkyl ring, a 5-7 membered heteroaryl with 1-3 heteroatoms selected from N, NR9, S and O, a 5-7 membered heterocycloalkyl with 1 or 2 heteroatoms selected from N, NR9, S and O, phenyl or naphthyl rings; or R11 and R12, together with the carbons to which they are attached, form a mono- or bicyclic heterocycloalkyl, of 5 to 10 saturated or unsaturated members, with 1-2 heteroatoms selected from N, NR9, S and O, optionally fused to a 5 to 7 membered mono- or bicyclic heteroaryl with 5 to 7 members, 1 to 3 heteroatoms selected from N, NR9, S and O, a 5 to 7 membered cycloalkyl ring, saturated or unsaturated or a phenyl ring or naphthyl; the dotted line represents an optional double bond; and n = 0-2, or a pharmaceutically acceptable salt thereof.

ARP000100325A 1999-01-27 2000-01-26 AMIDA-HYDROXAMIC ACID, ACETYLLENE, BETA-SULPHONAMIDE AND PHOSPHINIC ACID AS INHIBITORS OF TACE, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PHARMACEUTICAL COMPOSITION CONTAINING THEM AR035478A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US23908399A 1999-01-27 1999-01-27

Publications (1)

Publication Number Publication Date
AR035478A1 true AR035478A1 (en) 2004-06-02

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ARP000100325A AR035478A1 (en) 1999-01-27 2000-01-26 AMIDA-HYDROXAMIC ACID, ACETYLLENE, BETA-SULPHONAMIDE AND PHOSPHINIC ACID AS INHIBITORS OF TACE, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PHARMACEUTICAL COMPOSITION CONTAINING THEM

Country Status (16)

Country Link
EP (1) EP1147078A1 (en)
JP (1) JP2002535383A (en)
KR (1) KR20010089617A (en)
CN (1) CN1337944A (en)
AR (1) AR035478A1 (en)
AU (1) AU769410B2 (en)
BR (1) BR0007754A (en)
CA (1) CA2356345A1 (en)
CZ (1) CZ20012709A3 (en)
EA (1) EA200100808A1 (en)
HU (1) HUP0200605A3 (en)
IL (1) IL144321A0 (en)
NO (1) NO20013639D0 (en)
NZ (1) NZ512025A (en)
WO (1) WO2000044711A1 (en)
ZA (1) ZA200104508B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021489A2 (en) 2002-12-23 2005-03-10 Wyeth Holdings Corporation Acetylenic aryl sulfonate hydroxamic acid tace and matrix metalloproteinase inhibitors
US8129406B2 (en) * 2004-03-22 2012-03-06 Southern Research Institute Nonpeptide inhibitors of matrix metalloproteinases
FR2947268B1 (en) 2009-06-30 2011-08-26 Galderma Res & Dev NOVEL BENZENE-SULFONAMIDE COMPOUNDS, PROCESS FOR THE SYNTHESIS AND THEIR USE IN MEDICINE AND COSMETICS
FR2950057B1 (en) 2009-09-17 2011-08-26 Galderma Res & Dev NOVEL BENZENE CARBOXYLAMIDE COMPOUNDS, PROCESS FOR THEIR SYNTHESIS AND THEIR USE IN MEDICINE AND COSMETICS
WO2020070239A1 (en) 2018-10-04 2020-04-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Egfr inhibitors for treating keratodermas

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5514716A (en) * 1994-02-25 1996-05-07 Sterling Winthrop, Inc. Hydroxamic acid and carboxylic acid derivatives, process for their preparation and use thereof
TNSN97084A1 (en) * 1996-05-15 2005-03-15 Bayer Corp BIARYL ACETYLENES AS INHIBITORS OF METALLOPROTEINASE MATRICES
JP2001504809A (en) * 1996-10-16 2001-04-10 アメリカン・サイアナミド・カンパニー Preparation and use of ortho-sulfonamidoarylhydroxamic acids as inhibitors of matrix metalloproteinases and tace
US5977408A (en) * 1996-10-16 1999-11-02 American Cyanamid Company Preparation and use of β-sulfonamido hydroxamic acids as matrix metalloproteinase and TACE inhibitors
PL339730A1 (en) * 1997-10-06 2001-01-02 American Cyanamid Co Production and application of orthosulphonamidobicycloheteroaryl hydroxamic acids as matrix-type inhibitors of metaloproteinases and tace

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EP1147078A1 (en) 2001-10-24
JP2002535383A (en) 2002-10-22
AU2630600A (en) 2000-08-18
NO20013639L (en) 2001-07-24
HUP0200605A2 (en) 2002-07-29
ZA200104508B (en) 2002-09-02
HUP0200605A3 (en) 2005-05-30
NZ512025A (en) 2003-08-29
BR0007754A (en) 2001-11-13
CA2356345A1 (en) 2000-08-03
CZ20012709A3 (en) 2002-04-17
AU769410B2 (en) 2004-01-29
NO20013639D0 (en) 2001-07-24
IL144321A0 (en) 2002-05-23
CN1337944A (en) 2002-02-27
WO2000044711A1 (en) 2000-08-03
EA200100808A1 (en) 2001-12-24
KR20010089617A (en) 2001-10-06

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