AR015141A1 - ENDOTHELINE ANTAGONIST HETEROCICLIC DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THEM, THE USE OF THE SAME IN THE MANUFACTURE OF A MEDICINAL PRODUCT AND PROCEDURE FOR PREPARATION - Google Patents
ENDOTHELINE ANTAGONIST HETEROCICLIC DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THEM, THE USE OF THE SAME IN THE MANUFACTURE OF A MEDICINAL PRODUCT AND PROCEDURE FOR PREPARATIONInfo
- Publication number
- AR015141A1 AR015141A1 ARP980103833A AR015141A1 AR 015141 A1 AR015141 A1 AR 015141A1 AR P980103833 A ARP980103833 A AR P980103833A AR 015141 A1 AR015141 A1 AR 015141A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- alkylene
- hydrogen
- lower alkyl
- independently selected
- Prior art date
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Antagonistas de endotelina que comprende la formula (I) donde Z es -C(R18)(R19)- o -C(O)- donde R18 y R19 están independientemente seleccionados dehidrogeno y alquilo inferior; n es 0 o 1; R es -(CH2)m-W donde m es un entero de 0 a 6 y W es (a) -C(O)2-G donde G es hidrogeno o un grupo protector carboxi, (b) -PO3H2, (c)-P(O)(OH)E donde E es hidrogeno, alquilo inferior o arilalquilo, (d) -CN, (e) -C(O)NHR17 donde R17 es alquilo inferior, (f) alquilaminocarbonilo,(g) dialquilaminocarbonilo, (h) tetrazolilo, (i) hidroxi, (j)alcoxi, (k) sulfonamido, (l) -C(O)NHS(O)2R16 donde R16 es alquilo inferior, haloalquilo, arilo odialquilamino, (m) -S(O)2NHC(O)R16 donde R16 es tal como se ha definido más arriba, es formula (II), (n) es formula (III), (o) es formula (IV), (p) es formula(V), (q) es formula (VI), (r) es formula (VII), (s) es formula (VIII), (t) es formula (IX); R1 y R2 están independientemente seleccionados de hidrogeno, alquiloinferior, alquenilo, alquinilo, alcoxialquilo, alcoxicarbonilalquilo, hidroxialquilo, haloalquilo, haloalcoxialquilo, alcoxialcoxialquilo,tioalcoxialcoxialquilo, cicloalquilo, cicloalquialquilo, aminocarbonilalquilo, alquilaminocarbonilalquilo, dialquilaminocarbonilalquilo,aminocarbonilalquenilo,alquilaminocarbonilalquenilo, dialquilaminocarbonilalquenilo, hidroxialquenilo, arilo, arilalquilo, ariloxialquilo, arilalcoxialquilo, (N-alcanoil-N-alquil)aminoalquilo, alquilsulfonilamidoalquilo, heterociclico, (heterociclico)alquilo y (Raa)(Rbb)N-Rcc donde Raaes arilo o arilalquilo, Rbb es hidrogeno oalcanoilo y Rcc es alquileno, con la condicion de que uno o ambos de R1 y R2 son distinto de H; R3 es (a)R4-C-(O)-R5-, R4-R5a, R4-C(O)-R5-N(R6)-, R6-S(O)2-R7-o R26-S(O)-R27, donde R5 es (i) un enlace covalente, (ii) alquileno, (iii) alquenileno, (iv) -N(R20)R8- o R8a-N(R20)-R8 donde R8 y R8a están independientementeseleccionados del grupo que consiste en alquileno y alquenileno y R20 es hidrogeno, alquilo inferior, alquenilo, haloalquilo, alcoxialquilo,haloalcoxialquilo,cicloalquilo o cicloalquilalquilo o (v) -O-R9- o -R9a-O-R9- donde R9 y R9a están independientemente seleccionados de alquileno; R5a es (i) alquileno o (ii)Endothelin antagonists comprising formula (I) where Z is -C (R18) (R19) - or -C (O) - where R18 and R19 are independently selected from hydrogen and lower alkyl; n is 0 or 1; R is - (CH2) mW where m is an integer from 0 to 6 and W is (a) -C (O) 2-G where G is hydrogen or a carboxy protecting group, (b) -PO3H2, (c) - P (O) (OH) E where E is hydrogen, lower alkyl or arylalkyl, (d) -CN, (e) -C (O) NHR17 where R17 is lower alkyl, (f) alkylaminocarbonyl, (g) dialkylaminocarbonyl, ( h) tetrazolyl, (i) hydroxy, (j) alkoxy, (k) sulfonamido, (l) -C (O) NHS (O) 2R16 where R16 is lower alkyl, haloalkyl, aryl odyalkylamino, (m) -S (O ) 2NHC (O) R16 where R16 is as defined above, is formula (II), (n) is formula (III), (o) is formula (IV), (p) is formula (V), (q) is formula (VI), (r) is formula (VII), (s) is formula (VIII), (t) is formula (IX); R1 and R2 are independently selected from hydrogen, alquiloinferior, alkenyl, alkynyl, alkoxyalkyl, alkoxycarbonylalkyl, hydroxyalkyl, haloalkyl, haloalkoxyalkyl, alkoxyalkoxyalkyl, tioalcoxialcoxialquilo, cycloalkyl, cycloalkylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, aminocarbonylalkenyl, alquilaminocarbonilalquenilo, dialquilaminocarbonilalquenilo, hydroxyalkenyl, aryl, arylalkyl , aryloxyalkyl, arylalkoxyalkyl, (N-alkanoyl-N-alkyl) aminoalkyl, alkylsulfonylamidoalkyl, heterocyclic, (heterocyclic) alkyl and (Raa) (Rbb) N-Rcc where Raaes are aryl or arylalkyl, Rbb is hydrogenalkyl and Rcc is alkylene and Rcc is alkylene the condition that one or both of R1 and R2 are different from H; R3 is (a) R4-C- (O) -R5-, R4-R5a, R4-C (O) -R5-N (R6) -, R6-S (O) 2-R7- or R26-S ( O) -R27, where R5 is (i) a covalent bond, (ii) alkylene, (iii) alkenylene, (iv) -N (R20) R8- or R8a-N (R20) -R8 where R8 and R8a are independently selected of the group consisting of alkylene and alkenylene and R20 is hydrogen, lower alkyl, alkenyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, cycloalkyl or cycloalkylalkyl or (v) -O-R9- or -R9a-O-R9- where R9 and R9a are independently selected from alkylene; R5a is (i) alkylene or (ii)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/905,913 US6162927A (en) | 1994-08-19 | 1997-08-04 | Endothelin antagonists |
| US4895598A | 1998-03-27 | 1998-03-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR015141A1 true AR015141A1 (en) | 2001-04-18 |
Family
ID=40956433
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980103833 AR015141A1 (en) | 1997-08-04 | 1998-08-03 | ENDOTHELINE ANTAGONIST HETEROCICLIC DERIVATIVES, PHARMACEUTICAL COMPOSITION CONTAINING THEM, THE USE OF THE SAME IN THE MANUFACTURE OF A MEDICINAL PRODUCT AND PROCEDURE FOR PREPARATION |
Country Status (2)
| Country | Link |
|---|---|
| AR (1) | AR015141A1 (en) |
| CO (1) | CO5190718A1 (en) |
-
1998
- 1998-07-31 CO CO98043616A patent/CO5190718A1/en not_active Application Discontinuation
- 1998-08-03 AR ARP980103833 patent/AR015141A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CO5190718A1 (en) | 2002-08-29 |
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