AR016087A1 - 5-SUBSTITUTED DERIVATIVES-1,2,4-TIADIAZOLILO ANGIOGENESIS INHIBITORS, PROCEDURES FOR THEIR PREPARATION, ITS USE AS A MEDICINE, COMPOSITION PHARMACEUTICAL COMPOSITION, PROCEDURES FOR THE PREPARATION, INTERMEDIARY COMPOSITION AND PREPARATION PROCEDURE. - Google Patents

5-SUBSTITUTED DERIVATIVES-1,2,4-TIADIAZOLILO ANGIOGENESIS INHIBITORS, PROCEDURES FOR THEIR PREPARATION, ITS USE AS A MEDICINE, COMPOSITION PHARMACEUTICAL COMPOSITION, PROCEDURES FOR THE PREPARATION, INTERMEDIARY COMPOSITION AND PREPARATION PROCEDURE.

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Publication number
AR016087A1
AR016087A1 ARP980103020A ARP980103020A AR016087A1 AR 016087 A1 AR016087 A1 AR 016087A1 AR P980103020 A ARP980103020 A AR P980103020A AR P980103020 A ARP980103020 A AR P980103020A AR 016087 A1 AR016087 A1 AR 016087A1
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AR
Argentina
Prior art keywords
alkyl
preparation
alkyloxy
amino
composition
Prior art date
Application number
ARP980103020A
Other languages
Spanish (es)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR016087A1 publication Critical patent/AR016087A1/en

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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135—Nitrogen 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
    • A61K31/33—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
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/83—Thioacids; Thioesters; Thioamides; Thioimides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Derivados 5 sustituido-1,2,4-tiadiazolilo inhibidores de angiogénesis que tienen la formula I las formas de N-oxido, las sales de adicion de ácidofarmacéuticamente aceptables y las formas estereoquímicamente isoméricas de los mismos donde X es CH oN ; R1 es hidrogeno, alquilo C1-6, alquiloxi C1-6,alquiltio C1-6, amino, mono o di(alquilo C1-6)amino, Ar1, Ar1-NH-, cicloalquilo C3-6, hidroximetilo, o benciloximetilo; R2 es hidrogeno, alquilo C1-6 amino,aminocarbonilo, mono o di (alquilo C1-6)amino , alquiloxicarbonilo C1-6, alquilcarbonilamino C1-6, hidroxi o alquiloxi C1-6; R3, R4 y R5 están cada unoindependientemente seleccionados de hidrogeno, halo, alquilo C1-6, alquiloxi C1-6, trifluormetilo, nitro, amino, ciano, azido, alquiloxiC1-6, a lquilo C1-6,alquiltio C1-6, alquiloxicarbonilo C1-6, Het1; A es Ar2, Ar2-CH2-o Het2, Ar1 es fenilo, fenilo sustituido con 1, 2 o 3 sustituyentes cada uno de ellosindependientemente seleccionado de halo, alquilo C1-6, alquiloxi C1-6,trialometilo, ami no o nitro y Ar2 es fenilo substituido con 1, 2 o 3 substituyentes cadauno de ellos independientemente seleccionado de halo, alquilo C1-6, alquiloxi C1-6, trialometilo, amino o nitro, Het1 es un heterocíclico monocíclico queestáseleccionado de oxazo lilo,isoxazolilo,oxadiazolilo,tiazolilo,isotiazolilo,tidiazolilo o oxazolinilo, y cada heterocíclo monocíclico puede estar opcionalmentesustituido en un átomo de carbono de alquilo C1-4; y Het2 es un heterociclo monocíclicoque está seleccionado de f uranilo, tiofuranilo, oxadiazolilo,tiadiazolilo, piridinilo, pirimidinilo o pirazinilo y cada heterociclo monociclico puede estar opcionalmente sustituido en un átomo de carbono con uno o dossustituyentes cada uno de ellosindependientemente seleccio nado de halo, alquilo C1-4, alquilo C1-4 nitro o trifluormetilo procedimiento para su preparacion,composicion que los contienen, procedimiento para su preparacion, su uso como medicina, compuesto intermediario yprocedimiento para su preparacion.Substituted 5-1,2,4-thiadiazolyl angiogenesis inhibitor derivatives having formula I N-oxide forms, acid pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof where X is CH or N; R1 is hydrogen, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylthio, amino, mono or di (C1-6 alkyl) amino, Ar1, Ar1-NH-, C3-6 cycloalkyl, hydroxymethyl, or benzyloxymethyl; R2 is hydrogen, C1-6 alkyl amino, aminocarbonyl, mono or di (C1-6 alkyl) amino, C1-6 alkyloxycarbonyl, C1-6 alkylcarbonylamino, hydroxy or C1-6 alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6 alkyl, C1-6 alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6 alkyloxy, to C1-6 alkyl, C1-6 alkylthio, alkyloxycarbonyl C1-6, Het1; A is Ar2, Ar2-CH2- or Het2, Ar1 is phenyl, phenyl substituted with 1, 2 or 3 substituents each independently selected from halo, C1-6 alkyl, C1-6 alkyloxy, trialomethyl, ami no or nitro and Ar2 it is phenyl substituted with 1, 2 or 3 substituents each independently selected from halo, C1-6 alkyl, C1-6 alkyloxy, trialomethyl, amino or nitro, Het1 is a monocyclic heterocyclic which is selected from oxazoyl, isoxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, thidiazolyl or oxazolinyl, and each monocyclic heterocycle may be optionally substituted on a C1-4 alkyl carbon atom; and Het2 is a monocyclic heterocycle which is selected from furanyl, thiofuranyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl or pyrazinyl and each monocyclic heterocycle may be optionally substituted on a carbon atom with one or two substituents each independently selected halo alkyl, C1-4, C1-4 alkyl nitro or trifluoromethyl process for its preparation, composition containing them, procedure for its preparation, its use as medicine, intermediate compound and procedure for its preparation.

ARP980103020A 1997-06-24 1998-06-23 5-SUBSTITUTED DERIVATIVES-1,2,4-TIADIAZOLILO ANGIOGENESIS INHIBITORS, PROCEDURES FOR THEIR PREPARATION, ITS USE AS A MEDICINE, COMPOSITION PHARMACEUTICAL COMPOSITION, PROCEDURES FOR THE PREPARATION, INTERMEDIARY COMPOSITION AND PREPARATION PROCEDURE. AR016087A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP97201931 1997-06-24
US5300397P 1997-07-10 1997-07-10

Publications (1)

Publication Number Publication Date
AR016087A1 true AR016087A1 (en) 2001-06-20

Family

ID=26146629

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980103020A AR016087A1 (en) 1997-06-24 1998-06-23 5-SUBSTITUTED DERIVATIVES-1,2,4-TIADIAZOLILO ANGIOGENESIS INHIBITORS, PROCEDURES FOR THEIR PREPARATION, ITS USE AS A MEDICINE, COMPOSITION PHARMACEUTICAL COMPOSITION, PROCEDURES FOR THE PREPARATION, INTERMEDIARY COMPOSITION AND PREPARATION PROCEDURE.

Country Status (4)

Country Link
KR (1) KR100534621B1 (en)
AR (1) AR016087A1 (en)
NO (1) NO314804B1 (en)
TW (1) TW510901B (en)

Also Published As

Publication number Publication date
TW510901B (en) 2002-11-21
NO314804B1 (en) 2003-05-26
NO996392D0 (en) 1999-12-22
KR100534621B1 (en) 2005-12-08
KR20010013009A (en) 2001-02-26
NO996392L (en) 1999-12-22

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