摘要:
A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R--NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.1 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
摘要:
A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R.sup.1 NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.2 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
摘要:
The invention provides a nitroreductase, obtainable from a bacterium having the following characteristics as exemplified by examples isolated from Escherichia coli B and Bacillus amyloliquifaciens: 1) it is flavoprotein having a molecular weight in the range of 20-60 Kilodaltons; 2) it requires either NADH or NAD(P)H or analogues thereof as a cofactor; 3) it has a Km for NADH or NAD(P)H in the range of 1-100 .mu.M; and 4) it is capable of reducing either or both nitro groups of CB1954 and analogues thereof to a cytotoxic form e.g. the hydroxylamine. The sequence of one such nitroreductase is shown in Seq. ID No. 1. The nitroreductase may be conjugated to a tumor targeting agent such as a monoclonal antibody and used to convert prodrugs into active antitumor agents. Such prodrugs and drugs are also provided.
摘要:
Use of an orally or nasally available formulation of Tretazicar for poisoning vermin. An orally available or nasally available formulation of Tretazicar, wherein in the orally available formulation the Tretazicar is protected from acid hydrolysis, and provided that the formulation is not solid Tretazicar in a gelatin capsule. A formulation of Tretazicar in which the Tretazicar is protected from acid hydrolysis, wherein the formulation is present in a liquid form. A combination of Tretazicar and bait. A method of poisoning vermin comprising making available to the vermin an orally or nasally available formulation of Tretazicar and allowing the vermin to ingest or inhale the formulation of Tretazicar.
摘要:
Use of an orally or nasally available formulation of Tretazicar for poisoning vermin. An orally available or nasally available formulation of Tretazicar, wherein in the orally available formulation the Tretazicar is protected from acid hydrolysis, and provided that the formulation is not solid Tretazicar in a gelatin capsule. A formulation of Tretazicar in which the Tretazicar is protected from acid hydrolysis, wherein the formulation is present in a liquid form. A combination of Tretazicar and bait. A method of poisoning vermin comprising making available to the vermin an orally or nasally available formulation of Tretazicar and allowing the vermin to ingest or inhale the formulation of Tretazicar.
摘要:
A method of combating toxicity caused by an antifolate compound of Formula I, in an individual who has been administered the compound. The method comprises administering an enzyme that has carboxypeptidase G activity to the individual.
摘要:
A method and apparatus for configuring an appliance, such as a network node, for performing a service, such as communicating with a network, controlled by a service provider include inserting into an Ethernet port on the appliance an Ethernet couple on a device that is usually small compared to the appliance. The device is configured to send through the Ethernet couple without human intervention an Internet Protocol (IP) data packet that is directed to a logical port of an established standard, such as Hypertext Transfer Protocol (HTTP) port 80. The IP data packet includes appliance configuration data in a message form for the established standard, such as an HTTP POST. As a result, the appliance is configured automatically for performing the service controlled by the service provider.
摘要:
A method of combating a parasitic protozoal infection of a host organism, the method comprising administering tretazicar to the host organism. Tretazicar is the compound 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954), and the parasitic infection is preferably an infection of Trypanosoma cruzi, T. b. brucei, Leishmania spp. particularly L. infantum, Cryptosporidium or Giardia spp.
摘要:
A method and apparatus for configuring an appliance, such as a network node, for performing s service, such as communicating with a network, controlled by a service provider include inserting into an Ethernet port on the appliance an Ethernet couple on a device that is usually small compared to the appliance. The device is configured to send through the Ethernet couple without human intervention an Internet Protocol (IP) data packet that is directed to a logical port of an established standard, such as Hypertext Transfer Protocol (HTTP) port 80. The IP data packet includes appliance configuration data in a message form for the established standard, such as an HTTP POST. As a result, the appliance is configured automatically for performing the service controlled by the service provider.
摘要:
A method and apparatus for configuring an appliance, such as a network node, for performing a service, such as communicating with a network, controlled by a service provider include inserting into an Ethernet port on the appliance an Ethernet couple on a device that is usually small compared to the appliance. The device is configured to send through the Ethernet couple without human intervention an Internet Protocol (IP) data packet that is directed to a logical port of an established standard, such as Hypertext Transfer Protocol (HTTP) port 80. The IP data packet includes appliance configuration data in a message form for the established standard, such as an HTTP POST. As a result, the appliance is configured automatically for performing the service controlled by the service provider.