公开(公告)号：JPH0426699A

公开(公告)日：1992-01-29

申请号：JP13326390

申请日：1990-05-23

Applicant: TOSOH CORP

Inventor： OE MASATAKE ,  KATSUURA KIMIO ,  NAGATA YOSHIHIKO ,  ARAI TAKAHIRO ,  YAMAMOTO KINYA

IPC: A61K9/127 ,  C07C271/20 ,  C07J9/00 ,  C07J41/00

Abstract: NEW MATERIAL:A compound of formula I [R1-O- is cholesterol (cholesterin) or cholestanol; R2 is hydroxymethyl, alkyloxycarbonyl or lower mono or dialkylaminocarbonyl; R3 is lower aminoalkyl ]. EXAMPLE:N -benzyloxycarbonyllysinolcholesterolurethane. USE:An amino acid-based cationic surfactant (with high safety and good biodegradability). PREPARATION:A condensation is made between (A) a compound of formula II [R2' is carboxyl; R4 is protective group eliminable under acidic condition (reductively) for the terminal amino group of lower aminoalkyl group] and (B) a cholesterol haloformate or cholestanol haloformate of formula III(X is halogen; broken line means single or double bond).

公开(公告)号：JPH0426662A

公开(公告)日：1992-01-29

申请号：JP13326490

申请日：1990-05-23

Applicant: TOSOH CORP

Inventor： OE MASATAKE ,  KATSUURA KIMIO ,  NAGATA YOSHIHIKO ,  ARAI TAKAHIRO ,  YAMAMOTO KINYA

IPC: C07C231/02 ,  C07C231/12 ,  C07C233/17 ,  C07C233/31 ,  C07C233/36

Abstract: NEW MATERIAL:A basic amino acid acyl derivative of formula I (RICO is 13-20C saturated or unsaturated fatty acid residue; R2 is CH2OH, acyloxycarbonyl, CONH2, lower mono-dialkylaminocarbonyl; R3 is lower alkyl) and an acid adduct thereof. EXAMPLE:N -Palmitoyl lysinol. USE:An amino acid cationic surfactant having high safety, excellent bio- decomposability and a high function and particularly useful as a positive charge substance for liposome membranes. PREPARATION:A compound of formula II (R4 is lower aminoalkyl group whose terminal amino group is protected with a protecting group capable of being released under an acidic condition or under a reducing condition) is condensed with a compound of formula III (X is halogen) and a protecting group in the R4 group of the prepared novel compound of formula IV is removed to effectively provide the compound of formula I.

公开(公告)号：JPH03279394A

公开(公告)日：1991-12-10

申请号：JP7897290

申请日：1990-03-29

Applicant: TOSOH CORP

Inventor： HARA KAZUTOSHI ,  HORIE RYUICHI ,  KATSUURA KIMIO ,  NAKANO KOICHI

IPC: C07H15/04 ,  C07H15/10

Abstract: NEW MATERIAL:A compound expressed by formula I {R is H or lower acyl; X is NH3, NHCOCH3 or NH2; either R1 or R2 is H and the other is expressed by formula II [R3 is expressed by formula III (X1 is H and X2 is H, or X1 is OR5 and X2 is H, etc.); R4 is expressed by formula IV (X3 is H and X4 is H, or X3 and X4 are joined to form a double bond, etc.; R5 is H or acetyl, etc.); n and m are 10-25], etc.}. USE:A mammal is sensitized by said compound and produces antibody against glycolipid derivatives. PREPARATION:An oligosaccharide expressed by formula V (R8 is lower acyl; R9 is OCOCH3, F, Cl, Br, O-C(=NH)CCl3, SCH3 or OH) is reacted with lipid having long alkyl chain expressed by formula VI or formula VII (R6 and R7 are 10-25C alkyl).

公开(公告)号：JPH02304063A

公开(公告)日：1990-12-17

申请号：JP12225089

申请日：1989-05-16

Applicant: TOSOH CORP

Inventor： KUBO AKINORI ,  KITAHARA YOSHIYASU ,  MIYAKE TOSHIO ,  KATSUURA KIMIO

IPC: C07D215/40 ,  A61K31/47 ,  A61K31/535 ,  A61P31/12 ,  C07D401/04

Abstract: NEW MATERIAL:An 8-position nitrogen-substituted 5,6-hydroquinoline-5,6-dione shown by formula I [R1, R2 and R3 are H or 1 to 6C alkyl; A is CH2CH2, CH2 OCH2, CH2CHR8CH2 (R8 is H or 1 to 6C alkyl), and a case wherein R1, R2 and R3 are H and A is CH2CH2CH2 or CH2OCH2 is omitted]. USE:Useful as a reverse transcriptase effective as a medicine for infectious diseases of retrovirus, having low toxicity. PREPARATION:The subject substance can be produced by a well-know method, for example, 6-hydroxy-2-methylquinoline is dissolved in methanol and pyrrolidine and cupric acetate are added to the solution by cooling with ice while stirring. The mixture is stirred while introducing an oxygen gas. The solvent of the reaction solution is distilled away under reduced pressure to give the objective compound shown by the formula.