Takeda Chemical Industries, Inc.

Ryuji M Marumoto

Yoshiyasu Furukawa

Masao Tanabe

Koichi Igarashi

Kiyohisa Kawai

Tomoko Fujii

Shunsuke Shima

Susumu Iwasa

Yoshio Yoshioka

Reiko Sasada

Yoshio Taniyama

Naoki Yamamoto

Yoichi Sawa

Mikio Honjo

Katsuyoshi Kawazoe

Takumi Hamana

Yoshiyuki Kawakami

Lymphotoxin (LT) mutein (genetically-altered LT) is disclosed that has the following amino acid sequence, or a portion of an active portion of said protein, where 10 to 21 amino acids of LT being deleted from N-terminus and which has Pro or Phe at the N-terminus: ##STR1## Wherein R.sub.1 is Pro or Phe, R.sub.2 is a peptide chain represented by the following sequence:

DNA encoding recombinant human lymphotoxin

A compound of the formula: ##STR1## wherein R is a hydroxyl group which may be protected and Y is a purine base which may be protected, and the saltts thereof, which are useful as an antiviral agent.

Antiviral carbocyclic purine nucleosides

An animal cell line transformed with an expression vector for an animal cell, the expression vector which contains a DNA segment comprising:

Expression vector for animal cell line and use thereof

Novel N.sup.2 -substituted-2,6-diaminonebularines of the formula: ##STR1## wherein R is 2-pyridyl or 3-pyridyl, which may be substituted, or acid addition salts thereof have an excellent coronary vasodilator action.

2,6-Diaminonebularines, their production and use

Compounds of the formula ##STR1## wherein R is phenyl which may be substituted; or their acid addition salts, are produced in good yield by reacting a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3, independently of one another, are hydroxyl which may be protected, which is prepared in 2 or 3 steps from 5-amino-1-.beta.-D-ribofuranosylimidazole-4-carboxamide, with a compound of the formula ##STR3## wherein R has the same meaning as defined above and X is amino which may be substituted or lower alkylthio, and, if necessary subjecting the resulting compound to a treatment for removal of protective groups on its hydroxyls.

Production of 2,6-diaminonebularines

Novel N.sup.2 -substituted phenyl-2,6-diaminonebularines of the formula ##STR1## wherein either one of R.sup.1 and R.sup.2 is carbamoyl which may be substituted or acyl group and the other is hydrogen atom, halogen atom or lower alkoxyl group, and their acid addition salts have an excellent coronary vasodilator action.

2,6-Diaminonebularines

Compounds of the formula ##STR1## wherein R is a phenyl or cyclohexyl group which may be substituted by halogen, lower alkyl or lower alkoxy, or their acid addition salts, are produced in good yield by reacting a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3, independently of each other, are a hydroxyl group which may be proctected, which is prepared in 2 or 3 steps from 5-amino-1-.beta.-D-ribofuranosylimidazole-4-carboxamide, with a compound of the formula

Novel N.sup.2 -substituted phenyl-2,6-diaminonebularines of the formula ##STR1## wherein R.sup.1 is halogen, lower alkyl or lower alkoxy and R.sup.2 is hydrogen, halogen, lower alkyl or lower alkoxy, and their acid addition salts have excellent coronary vasodilator action.

Isoxazolo[3,4-d]pyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, respectively, are hydrogen, lower alkyl, cycloalkyl, or aryl which may be substituted by halogen, are useful as antiinflammatory-analgesic drugs, and the industrially feasible production thereof is provided.

Isoxazolo[3,4-d]pyrimidines

Isoxazolo[3,4-d]pyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 respectively, are hydrogen, lower alkyl, cycloalkyl, or aryl which may be substituted by halogen, are useful as antiinflammatory-analgesic drugs, and the industrially feasible production thereof is provided.

Isoxazolo[3,4-d]pyrimidines useful as antiinflammatory-analgesic agents

Novel 2,6-diaminonebularine derivatives of the formula ##SPC1## Wherein R is a phenyl or cyclohexyl group which may be substituted with lower alkyl, lower alkoxy or halogen, and pharmaceutically acceptable salts thereof, exhibit excellent pharmacological acitivity such as strong and prolonged coronary dilating and platelet aggregation inhibitory actions.

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Toyonaka, Japan

Ryuji M Marumoto