AR035610A1 - Pirimidin sulfamidas, intermediarios, composiciones farmaceuticas, un procedimiento para su manufactura, el uso de dichos compuestos para la produccion de composiciones farmaceuticas - Google Patents

Pirimidin sulfamidas, intermediarios, composiciones farmaceuticas, un procedimiento para su manufactura, el uso de dichos compuestos para la produccion de composiciones farmaceuticas

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Publication number
AR035610A1
AR035610A1 ARP010105818A ARP010105818A AR035610A1 AR 035610 A1 AR035610 A1 AR 035610A1 AR P010105818 A ARP010105818 A AR P010105818A AR P010105818 A ARP010105818 A AR P010105818A AR 035610 A1 AR035610 A1 AR 035610A1
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AR
Argentina
Prior art keywords
lower alkyl
heteroaryl
amino
aryl
cycloalkyl
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ARP010105818A
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English (en)
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Actelion Pharmaceuticals Ltd
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Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of AR035610A1 publication Critical patent/AR035610A1/es

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    • 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
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    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
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    • 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
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract

Pirimidin-sulfamidas, que comprenden compuestos de la fórmula general (1), en la cual R1 representa arilo, arilo-alquilo inferior, heteroarilo, heteroarilo-alquilo inferior, cicloalquilo, cicloalquilo-alquilo inferior, heterociclilo, heterociclilo-alquilo inferior, alquilo inferior, hidrógeno o pueden formar un anillo heterociclilo o cicloalquilo conjuntamente con R6; R2 representa -CH3, -(CH2)n-Y-Ra, -(CH2)m-C:::C-(CH2)p-Z-Ra, -(CH2)k-C(Rb)=CRcRd, -CH2-tetrahidrofurano-2-ilo; R3 representa arilo, heteroarilo; R4 representa hidrógeno, trifluormetilo, alquilo inferior, alquilo inferior-amino, alquiloxi inferior, alquiloxi inferior-alquiloxi inferior, hidroxi-alcoxi inferior, alquilo inferior-sulfinilo, alquiltio inferior, alquiltio inferior-alquilo inferior, hidroxi-alquilo inferior, alquilo inferior-oxi-alquilo inferior, hidroxi-alquilo inferior-oxi-alquilo inferior alquilo, hidroxi-alquilo inferior-amino, alquilo inferior-amino-alquilo inferior, amino, di-alquilo inferior-amino, [N-(hidroxi-alquilo inferior)-N-(alquilo inferior)]-amino, arilo, aril-amino, aril-alquilo inferior-amino, aril-tio, aril-alquilo inferior-tio, ariloxi, aril-alquilo inferior-oxi, aril-alquilo inferior, aril-sulfinilo, heteroarilo, heteroaril-oxi, heteroaril-alquilo inferior-oxi, heteroaril-amino, heteroaril-alquilo inferior-amino, heteroaril-tio, heteroaril-alquilo inferior-tio, heteroaril-alquilo inferior, heteroaril-sulfinilo, heterociclilo, heterociclil-alquilo inferior-oxi, heterociclil-oxi, heterociclil-amino, heterociclil-alquilo inferior-amino, heterociclil-tio, hetrociclil-alquilo inferior-tio, heterociclil-alquilo inferior, heterociclil-sulfinilo, cicloalquilo, cicloalquil-oxi, cicloalquil-alquilo inferior-oxi, cicloalquil-amino, cicloalquil-alquilo inferior-amino, cicloalquil-tio, cicloalquil-alquilo inferior-tio, cicloalquil-alquilo inferior, cicloalquil-sulfinilo; R6 representa hidrógeno, alquilo inferior, o puede formar una anillo heterociclilo o cicloalquilo conjuntamente con R1; X representa oxígeno, azufre, -CH2- o un enlace; Y representa un enlace, -O-, -NH-, -NH-SO2-, -NH-SO2-NH-, O-CO-, -CO-O-, -O-CO-NH-, -NH-CO-O, -NH-CO-NH-; Z representa oxígeno o un enlace; k representa los números enteros 1, 2, 3, 4, 5, o 6; n representa los números enteros 2, 3, 4, 5 o 6; m representa los números enteros 1, 2, 3, 4 o 5; p representa los números enteros 0(cero), 1, 2, o 3 y si p representa el número entero 0 (cero), Z no puede representar oxígeno; Ra representa arilo, heteroarilo, alquilo inferior, cicloalquilo, hidrógeno; Rb y Rc representan independientemente hidrógeno o alquilo inferior; Rd representa hidrógeno, alquilo inferior, arilo, heteroarilo; y los enantiómeros ópticamente puros, las mezclas de enantiómeros tales como por ejemplo racematos, diastereómeros ópticamente puros, mezclas de diastereómeros, racematos diastereoméricos, mezclas de racematos diastereoméricos y las meso-formas y sales de las mismas farmacéuticamente aceptables, intermediarios, composiciones farmacéuticas, un procedimiento para su manufactura, el uso de dichos compuestos para la producción de composiciones farmacéuticas, como antagonistas receptores de endotelina, para el tratamiento de desórdenes que están asociados con un rol de la endotelina, especialmente desórdenes circulatorios, tales como hipertensión, isquemia, vasoespasmo y angina pectoris, hiperlipidemia, desórdenes proliferativos tales como cáncer, migrana y desórdenes inflamatorios.
ARP010105818A 2000-12-18 2001-12-14 Pirimidin sulfamidas, intermediarios, composiciones farmaceuticas, un procedimiento para su manufactura, el uso de dichos compuestos para la produccion de composiciones farmaceuticas AR035610A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP0012890 2000-12-18

Publications (1)

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AR035610A1 true AR035610A1 (es) 2004-06-16

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ARP010105818A AR035610A1 (es) 2000-12-18 2001-12-14 Pirimidin sulfamidas, intermediarios, composiciones farmaceuticas, un procedimiento para su manufactura, el uso de dichos compuestos para la produccion de composiciones farmaceuticas

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US (2) US7094781B2 (es)
EP (2) EP1345920B1 (es)
JP (1) JP4245130B2 (es)
KR (1) KR100819668B1 (es)
CN (1) CN100432070C (es)
AR (1) AR035610A1 (es)
AT (1) ATE323079T1 (es)
AU (1) AU2002227984B8 (es)
BE (1) BE2014C019I2 (es)
BR (1) BRPI0116237B8 (es)
CA (1) CA2431675C (es)
CY (2) CY1105060T1 (es)
DE (1) DE60118782T2 (es)
DK (1) DK1345920T3 (es)
ES (1) ES2260318T3 (es)
FR (1) FR14C0017I2 (es)
HU (1) HU229403B1 (es)
IL (2) IL155805A0 (es)
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MX (1) MXPA03004780A (es)
MY (1) MY129150A (es)
NL (1) NL300672I2 (es)
NO (2) NO324952B1 (es)
NZ (1) NZ525614A (es)
PT (1) PT1345920E (es)
WO (1) WO2002053557A1 (es)
ZA (1) ZA200303695B (es)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0116237B8 (pt) * 2000-12-18 2021-05-25 Actelion Pharmaceuticals Ltd "composto de sulfamida, composição farmacêutica contendo o mesmo e seu uso como medicamento antagonista de receptor de endotelina".
EP2198867A1 (en) * 2001-12-07 2010-06-23 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as GSK-3 inhibitors
CN100379730C (zh) * 2002-12-02 2008-04-09 埃科特莱茵药品有限公司 嘧啶-磺酰胺及其作为内皮素受体拮抗剂的应用
EP1725540B1 (en) 2004-03-05 2012-09-12 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists
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