摘要:
Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要:
Peptides comprising the effective portion of human brain natriuretic peptide are provided in pharmaceutical compositions and methods to effect vasodilation and/or natriuresis.
摘要:
The cDNA sequence encoding porcine brain natriuretic peptide and related genes encoding canine and human peptides with natriuretic activity are disclosed. The gene is shown to make accessible the DNAs encoding analogous natriuretic peptides in other vertebrate species. The genes encoding these NPs can be used to effect modifications of the sequence to produce alternate forms of the NPs and to provide practical amounts of these proteins. The NPs of the invention can also be synthesized chemically. The invention peptides have the formula: R1-Cys-Phe-Gly-Arg- Arg/ - Leu/ -Asp-Arg- Lys Met (1) Ile- Gly/ -Ser- Leu/ -Ser-Gly-Leu-Gly-Cys-R-2 Ser Ser wherein R1 is selected from the group consisting of: (H); Gly-; Ser-Gly-; Asp/ Lys/ -Ser-Gly-; Gly Arg/ Asp/ His/ - Lys/ -Ser-Gly-; Gln Gly Arg/ Asp/ Met/ - His/ - Lys/ -Ser-Gly-; Val Gln Gly Arg/ Asp/ Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly Arg/ Asp/ Lys- Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly Arg/ Asp/ Pro-Lys- Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly Arg/ Asp/ Ser-Pro-Lys- Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly or a 10- to 109-amino acid sequence shown as the native upstream sequence for porcine, canine or human BNP in FIG. 8, or a composite thereof; R2 is (OH), NH2, or NR′R″ wherein R′ and R″ are independently lower alkyl (1-4C) or is Asn/ Lys Asn/ -Val Lys Asn/ -Val-Leu Lys Asn/ -Val-Leu-Arg Lys Asn/ -Val-Leu-Arg- Arg/ Lys Lys Asn/ -Val-Leu-Arg- Arg/ - Tyr/ Lys Lys His or the amides (NH2 or NR′R″) thereof, with the proviso that if formula (1) is R1-Cys-Phe-Gly-Arg-Arg-Leu-Asp-Arg- Ile-Gly-Ser-Leu-Ser-Gly-Leu-Gly-Cys-R2 and R1 is Asp-Ser-Gly-, R2 cannot be Asn-Val-Leu-Arg-Arg-Tyr. The peptides of the invention can be formulated into pharmaceutical compositions and used to treat conditions associated with high extracellular fluid levels, especially congestive heart failure.
摘要:
This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
摘要:
The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors: In formula (I), W is carbon or nitrogen, wherein at least one W is a carbon; and Y is nitrogen, oxygen, or sulfur. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.
摘要:
Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.
摘要:
Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.
摘要:
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要:
Ketoheterocyclic compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are usefull in vitro or in vivo for preventing or treating coagulation disorders.
摘要:
Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.