AR016071A1 - ENDOTHELINE ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND USE OF SUCH COMPOUNDS TO PREPARE MEDICINES - Google Patents
ENDOTHELINE ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND USE OF SUCH COMPOUNDS TO PREPARE MEDICINESInfo
- Publication number
- AR016071A1 AR016071A1 ARP980102851A ARP980102851A AR016071A1 AR 016071 A1 AR016071 A1 AR 016071A1 AR P980102851 A ARP980102851 A AR P980102851A AR P980102851 A ARP980102851 A AR P980102851A AR 016071 A1 AR016071 A1 AR 016071A1
- Authority
- AR
- Argentina
- Prior art keywords
- hydrogen
- lower alkyl
- alkylene
- haloalkyl
- alkenylene
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/02—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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto que comprende la formula (I), en donde: R es -(CH2)m-W, en donde m es un entero desde 0-6 y W es (a)-C(O)2-G, (b)-PO3H2,(c) -P(O)(OH)E,(d) -CN(e)-C(O)NHR17, alquilaminocarbonilo, dialquilaminocarbonilo, tetrazolilo, hidroxi, alcoxi, sulfonamido, -C(O)NHS(O)2R16, -S(O)2NHC(O)R16, o se selecciona entrelas formulas (n) a (u); G es hidrogeno o un grupo protector de carboxi; E es hidrogeno, alquilo inferior o arilalquilo; R17 es alquilo inferior; R16 es alquiloinferior, haloalquilo, arilo o dialquilamino; R1 y R2 son independientemente seleccionados de hidrogeno, alquilo inferior, alquenilo, alquinilo, alcoxialquilo,alcoxicarbonilalquilo, hidroxialquilo, haloalquilo, haloalcoxialquilo, alcoxialcoxialquilo, tioalcoxialcoxialquilo, cicloalquilo, cicloalquilalquilo,aminocarbonilalquilo, alquilaminocarbonilalquilo, dialquilaminocarbonilalquilo, aminocarbonilalquenilo, alquilaminocarbonilalquenilo, dialquilaminocarbonilalquenilo, hidroxialquenilo, arilo, arilalquilo, ariloxialquilo,arilalcoxialquilo, heterocíclico, alquilo(heterocíclico) y (Raa)(Rbb)N-Rcc-, en donde Raa esarilo o arilalquilo, Rbb es hidrogeno o alcanoílo, y Rcc es alquileno, con la condicion de que uno o ambos de R1 y R2 no es hidrogeno; R3 es R4-C(O)-R5, oR6-S(O)2-R7-, en donde R5 es un enlace covalente, alquileno, alquenileno, -N(R20)-R8- o -R8a-N(R20)-R8-, o -O-R9 o -R9a-O-R9-; en donde R8 y R8a sonindependientemente alquileno o alquenileno; R20 es hidrogeno, alquilo inferior, alquenilo, haloalquilo, alcoxialquilo, haloalcoxialquilo, cicloalquilo ocicloalquilalquilo; y R9 y R9a son independientemente alquileno; R7 es: un enlace covalente, alquileno, alquenileno o -N(R21)- R10 o -R10a-N(R21)-R10, en dondeR10 y R10a son independientemente seleccionados entre alquileno y alquenileno, y R21 es hidrogeno, alquilo inferior, alquenilo, haloalquilo, alcoxialquilo,haloalcoxialquilo, arilo o arilalquilo; R4 y R6 tienen la formula (II), en donde R11 y R12 son independientemente alquilo inferior, ciano,alcoxi, halo,haloalquilo o fenilo, y R13, R14 y R15 independientemente se seleccionan entre hidrogeno, alquilo inferior, hidroxi, amino, alcoxi, arilo, heterocíclico, halo,A compound comprising formula (I), wherein: R is - (CH2) mW, where m is an integer from 0-6 and W is (a) -C (O) 2-G, (b) - PO3H2, (c) -P (O) (OH) E, (d) -CN (e) -C (O) NHR17, alkylaminocarbonyl, dialkylaminocarbonyl, tetrazolyl, hydroxy, alkoxy, sulfonamido, -C (O) NHS (O ) 2R16, -S (O) 2NHC (O) R16, or formulas (n) to (u) are selected from; G is hydrogen or a carboxy protecting group; E is hydrogen, lower alkyl or arylalkyl; R17 is lower alkyl; R16 is lower alkyl, haloalkyl, aryl or dialkylamino; R1 and R2 are independently selected from hydrogen, lower alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxycarbonylalkyl, hydroxyalkyl, haloalkyl, haloalkoxyalkyl, alkoxyalkoxyalkyl, tioalcoxialcoxialquilo, cycloalkyl, cycloalkylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, aminocarbonylalkenyl, alquilaminocarbonilalquenilo, dialquilaminocarbonilalquenilo, hydroxyalkenyl, aryl, arylalkyl, aryloxyalkyl, arylalkoxyalkyl, heterocyclic, alkyl (heterocyclic) and (Raa) (Rbb) N-Rcc-, wherein Raa isaryl or arylalkyl, Rbb is hydrogen or alkanoyl, and Rcc is alkylene, with the proviso that one or both of R1 and R2 is not hydrogen; R3 is R4-C (O) -R5, oR6-S (O) 2-R7-, where R5 is a covalent bond, alkylene, alkenylene, -N (R20) -R8- or -R8a-N (R20) -R8-, or -O-R9 or -R9a-O-R9-; wherein R8 and R8a are independently alkylene or alkenylene; R20 is hydrogen, lower alkyl, alkenyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, cycloalkyl or cycloalkylalkyl; and R9 and R9a are independently alkylene; R7 is: a covalent bond, alkylene, alkenylene or -N (R21) -R10 or -R10a-N (R21) -R10, where R10 and R10a are independently selected from alkylene and alkenylene, and R21 is hydrogen, lower alkyl, alkenyl , haloalkyl, alkoxyalkyl, haloalkoxyalkyl, aryl or arylalkyl; R4 and R6 have the formula (II), wherein R11 and R12 are independently lower alkyl, cyano, alkoxy, halo, haloalkyl or phenyl, and R13, R14 and R15 are independently selected from hydrogen, lower alkyl, hydroxy, amino, alkoxy , aryl, heterocyclic, halo,
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US87718797A | 1997-06-17 | 1997-06-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR016071A1 true AR016071A1 (en) | 2001-06-20 |
Family
ID=25369437
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP980102851A AR016071A1 (en) | 1997-06-17 | 1998-06-16 | ENDOTHELINE ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND USE OF SUCH COMPOUNDS TO PREPARE MEDICINES |
Country Status (8)
Country | Link |
---|---|
AR (1) | AR016071A1 (en) |
AU (1) | AU7826398A (en) |
BG (1) | BG103986A (en) |
HU (1) | HUP0002681A3 (en) |
NO (1) | NO996244L (en) |
PL (1) | PL348667A1 (en) |
WO (1) | WO1998057933A1 (en) |
ZA (1) | ZA985209B (en) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7291626B1 (en) | 1998-04-09 | 2007-11-06 | John Hopkins University School Of Medicine | Inhibitors of hedgehog signaling pathways, compositions and uses related thereto |
EP1728797A3 (en) | 1999-10-13 | 2011-03-02 | Johns Hopkins University School of Medicine | Regulators of the hedgehog pathway, compositions and uses related thereto |
US6552016B1 (en) | 1999-10-14 | 2003-04-22 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
EP1227805B2 (en) * | 1999-10-14 | 2011-02-23 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
AR044510A1 (en) * | 2003-04-14 | 2005-09-14 | Merck & Co Inc | PROCEDURE AND INTERMEDIATES TO PREPARE CARBOXILIC ACIDS OF PIRROLIDINE |
CN114507143A (en) * | 2022-02-26 | 2022-05-17 | 江苏壹药新材料有限公司 | Synthesis method of 2-ethyl-1-fluoro-4-nitrobenzene |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2517691A1 (en) * | 1994-08-19 | 1996-02-29 | Abbott Laboratories | Endothelin antagonists |
BR9707394A (en) * | 1996-02-13 | 1999-04-06 | Abbott Lab | Derivatives of 4- (benzo-1,3-dioxolyl) pyrrolidine-3-carboxylic acid as endothelin antagonists |
-
1998
- 1998-06-08 HU HU0002681A patent/HUP0002681A3/en unknown
- 1998-06-08 AU AU78263/98A patent/AU7826398A/en not_active Abandoned
- 1998-06-08 WO PCT/US1998/011821 patent/WO1998057933A1/en not_active Application Discontinuation
- 1998-06-08 PL PL98348667A patent/PL348667A1/en unknown
- 1998-06-15 ZA ZA985209A patent/ZA985209B/en unknown
- 1998-06-16 AR ARP980102851A patent/AR016071A1/en unknown
-
1999
- 1999-12-10 BG BG103986A patent/BG103986A/en unknown
- 1999-12-16 NO NO996244A patent/NO996244L/en not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
NO996244L (en) | 2000-01-12 |
BG103986A (en) | 2000-08-31 |
PL348667A1 (en) | 2002-06-03 |
HUP0002681A2 (en) | 2001-08-28 |
ZA985209B (en) | 1999-01-06 |
NO996244D0 (en) | 1999-12-16 |
AU7826398A (en) | 1999-01-04 |
HUP0002681A3 (en) | 2001-09-28 |
WO1998057933A1 (en) | 1998-12-23 |
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