摘要:
The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.
摘要:
Provided is a subscriber-side communication device including a subscriber-side processing unit that continuously performs signal processing regardless of computer restart and includes a transmission processing unit that performs a data transmission process according to transmission control information contained in a received signal from the office-side communication device. Also provided is an office-side communication device including an office-side processing unit that continuously performs signal processing regardless of computer restart, and a transmission control information computing unit that computes transmission control information for each subscriber-side communication device, the office-side processing unit including a transmission control information storing unit that stores transmission control information of each subscriber-side communication device computed by the transmission control information computing unit, and a transmission control processing unit that performs a transmission control process with each subscriber-side communication device by using the transmission control information of each subscriber-side communication device stored in the transmission control information storing unit.
摘要:
Disclosed is a process for preparing 2.beta.-substituted-methylpenicillin derivative of the formula ##STR1## wherein R is H or carboxyl protecting group, R.sub.1 is H or halo, R.sub.2 is H, lower alkyl, lower alkoxy, halogen, azido, lower alkylthio, phthalimide or a group --NHR.sub.3 (wherein R.sub.3 is H or acyl), and --N Y is an optionally substituted monocyclic or bicyclic heterocyclic group having 1 to 4 nitrogen atoms in the ring structure, the process comprising reacting a compound of the formula ##STR2## wherein X is Cl or Br, and R, R.sub.1 and R.sub.2 are as defined above with a heterocyclic compound of the formula ##STR3## wherein --N Y is as defined above.
摘要:
Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.
摘要:
An analgesic composition containing as active ingredient a piperazine derivative represented by the general formula (1) ##STR1## wherein R.sub.1 represents a cyclopropylmethyl group, an isopropyl group or an allyl group and R.sub.2 represents a phenyl group having as substituent a halogen atom or a trifluoromethyl group.
摘要:
A tubular casing for sausage, ham or like processed meat mass is coated internally with a water-soluble complex chromium compound with a view to improved peelability, among other purposes, of the casing from the meat mass encased therein. The complex chromium compound may first be diluted with water, with the pH of the resulting aqueous solution regulated as required by the addition of a slight amount of caustic soda or the like. The thus-prepared coating fluid is coated in a suitable fashion on the internal surface of the tubular meat casing, which may be either cellulosic or fibrous, and the coated casing is then dried as by hot drafts of air.
摘要:
Provided is a subscriber-side communication device including a subscriber-side processing unit that continuously performs signal processing regardless of computer restart and includes a transmission processing unit that performs a data transmission process according to transmission control information contained in a received signal from the office-side communication device. Also provided is an office-side communication device including an office-side processing unit that continuously performs signal processing regardless of computer restart, and a transmission control information computing unit that computes transmission control information for each subscriber-side communication device, the office-side processing unit including a transmission control information storing unit that stores transmission control information of each subscriber-side communication device computed by the transmission control information computing unit, and a transmission control processing unit that performs a transmission control process with each subscriber-side communication device by using the transmission control information of each subscriber-side communication device stored in the transmission control information storing unit.
摘要:
A method of manufacturing substance GM-95 having general formula [I], comprising (a) deprotecting a macrocyclic compound having general formula [II] (wherein, R1's are the same or different and each represents a lower alkyl group, and R2 represents a thiol protecting group) by removing acetal protecting groups (the R1's) thereof, and forming an oxazole ring through an intramolecular cyclization reaction between produced formyl group and an amide group, and (b) deprotecting a resulting macrocyclic compound having general formula [III] (wherein, R2 is as mentioned above) by removing the thiol protecting group (R2) thereof, and forming a thiazoline ring through an intramolecular cyclization reaction between a thiol group thus produced and an amide group.
摘要:
This invention provides a compound having both IL-4 production inhibitory activity and PDE (IV) inhibitory activity, represented by formula (I): and a pharmaceutical composition or a therapeutic agent for acute and chronic inflammatory diseases and an anti-allergic or anti-inflammatory agent, each of which comprising an effective amount of the compound and a pharmacological carrier. It also provides use of the compound of formula (I) for the production of the aforementioned pharmaceutical composition or therapeutic agent for acute and chronic inflammatory diseases and anti-allergic or anti-inflammatory agent, and a method for treating acute and chronic inflammatory diseases.
摘要:
The invention relates an epoxysuccinamide derivative represented by a formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl or aminoalkyl group, R.sup.2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R.sup.3 and R.sup.4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.