公开(公告)号：JPH06306064A

公开(公告)日：1994-11-01

申请号：JP9425693

申请日：1993-04-21

Applicant: TOSOH CORP

Inventor： IDE TERUHIKO ,  FUJIWARA MASAHISA ,  HANAZAKI YASUAKI ,  WATANABE HIROYUKI ,  KATSUURA KIMIO

IPC: A01N43/832 ,  A01N43/82 ,  A61K31/41 ,  A61K31/433 ,  A61P31/04 ,  A61P31/10 ,  C07D285/10

Abstract: PURPOSE:To obtain the novel compound, excellent in antifungal activity and useful as an agrichemical, an industrial and a medical germicides. CONSTITUTION:The compound is expressed by formula I (X, Y and Z are H, halogen, 1-6C alkyl, 1-4C alkoxy or nitro; R is 1-6C alkyl), e.g. 2-methyl-4-(2,6- dichlorophenyl)1,2,5-thiadiazol-3(2H)-one. This compound expressed by formula I is obtained by reacting one equiv. compound expressed by formula II with 1-20 equiv. alkylating agent at 30-180 deg.C for 1min to 24hr.

公开(公告)号：JPH06306062A

公开(公告)日：1994-11-01

申请号：JP9425393

申请日：1993-04-21

Applicant: TOSOH CORP

Inventor： HANAZAKI YASUAKI ,  WATANABE HIROYUKI ,  KATSUURA KIMIO

IPC: C07D285/10

Abstract: PURPOSE:To obtain the novel derivative useful as an organic intermediate and an intermediate for medicines and pesticides. CONSTITUTION:The derivative is expressed by formula I (X and Y are H, halogen, 1-6C alkyl, 1-4C alkoxy, nitro, trifluoromethyl, carboxyl, 1-4C alkoxycarbonyl, naphthyl or tetrahydronaphthyl), e.g. 3-hydroxy-4-(4- methoxyphenoxy)-1,2,5-thiadiazole. This compound expressed by formula I is obtained by reacting a 3-chloro-1,2,5-thiadiazole derivative expressed by formula II with a base [an organic base (pyridine, triethylamine, etc.) or an inorganic base (sodium hydroxide, potassium hydroxide, etc.), etc.] in the presence or absence of an organic solvent [aromatic hydrocarbons (benzene, toluene, xylene, etc.), ethers (diethyl ether, dioxane, etc.), etc.] in water at 30-80 deg.C for 1-6hr.

公开(公告)号：JPH03280894A

公开(公告)日：1991-12-11

申请号：JP8085690

申请日：1990-03-30

Applicant: TOSOH CORP

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

IPC: G01N33/574 ,  A61K39/395 ,  C12N5/10 ,  C12N5/20 ,  C12N15/02 ,  C12N15/06 ,  C12P21/08 ,  C12R1/91 ,  G01N33/577

Abstract: NEW MATERIAL:A monoclonal antibody capable of recognizing a glycolipid derivative expressed by the formula. USE:A detecting reagent for cancer-related saccharide chain antigens and treating agent for cancer. PREPARATION:For example, the glycolipid derivative expressed by the formula is adsorbed in an emulsion of monophosphoryl-lipid A and dimycolic acid trehalose and repeatedly administered into the abdominal cavity of BALB/c mouse for immunization. After the final immunization, splenic cells are recovered and then fused to mouse myelomatous cells using polyethylene glycol, etc., and a clone capable of producing an antibody specifically binding to the glycolipid derivative expressed by the formula is selected from the produced hybridoma according to the Kohler method, etc., and cloned by a limiting dilution method, etc., to provide a cloned hybridoma. The resultant hybridoma is subsequently cultured to afford the objective monoclonal antibody capable of recognizing the glycolipid derivative expressed by the formula.

公开(公告)号：JPH03275694A

公开(公告)日：1991-12-06

申请号：JP7565290

申请日：1990-03-27

Applicant: TOSOH CORP

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

IPC: C07H15/04 ,  C07H15/10

Abstract: NEW MATERIAL:A compound shown by formula I {R is H or lower acyl; X is N3, NHCOCH3 or NH2; on of R1 and R2 is H and the other is group shown by formula II [R3 is group shown by formula III (X1 and X2 are H, etc.; n is 10-25); R4 is group shown by formula IV (X3 and X4 are H, etc.; m is 10-25), etc.]}. USE:A compound sensitizing a mammal and forming an antibody. PREPARATION:The azide group of glycolipid derivative shown by formula V (one or R12 and R13 is H and the other is acetyl; X5 is group shown by formu la II, etc.), converted into an amino group, the amino group is acetylated, option ally deacetylated and deprotection such as debenzoylation is carried out.

公开(公告)号：JP2000026456A

公开(公告)日：2000-01-25

申请号：JP19389798

申请日：1998-07-09

Applicant: TOSOH CORP ,  YOSHITOMI PHARMACEUTICAL

Inventor： YAMAMOTO TAKASHI ,  TOKUNAGA TAKUMI ,  ITO HIROYUKI ,  KONO KAZUHISA ,  HANAZAKI YASUAKI ,  KATSUURA KIMIO ,  SHINSAN HIROSHI ,  EGI YASUHARU ,  ISHIDA NAOMICHI ,  INOUE YOSHIHISA ,  YAMAUCHI KENJI

IPC: C07D333/36 ,  A61K31/38 ,  A61K31/381 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07F7/10

Abstract: PROBLEM TO BE SOLVED: To obtain a new benzylamine derivative having a high safety and an excellent inhibitory activity toward a squalene epoxybase, and useful for the prevention and treatment of hypercholesterolemia, etc. SOLUTION: This new benzylamine derivative is a compound of formula I [R1 is a (substituted) phenyl or a heterocyclic ring; L1 to L4 are each O, S, NR8 (R8 is H or a lower alkyl) or the like; R2 is H or a (halogen substituted) lower alkyl; R3 to R6 are each H or a halogen; R3 with R5, and R4 with R6 form single bonds; R7 is H, a halogen, a lower alkyl, a lower alkenyl or the like], e.g. (E)-N-ethyl-N-(6,6-dimethyl-2-hepten-4-ynyl)-3-[2-(N'-methyl-N'- thiophen-3-yl-amino)ethyl]oxy-benzylamine. Further, the compound of formula I is obtained by reacting a compound of formula II (X is an eliminable group) with an amine derivative of formula III in an inert solvent such as tetrahydrofuran, etc., in the presence of a condensation agent.

公开(公告)号：JP2000026453A

公开(公告)日：2000-01-25

申请号：JP19394598

申请日：1998-07-09

Applicant: TOSOH CORP

Inventor： YAMAMOTO TAKASHI ,  TOKUNAGA TAKUMI ,  ITO HIROYUKI ,  KONO KAZUHISA ,  HANAZAKI YASUAKI ,  KATSUURA KIMIO

IPC: C07D333/20 ,  C07D333/24

Abstract: PROBLEM TO BE SOLVED: To obtain a new 3-aminomethylthiophene derivative useful as a synthetic intermediate, etc., of a therapeutic agent of hypercholesterolemia, hyperlipidemia, arteriosclerosis, etc. SOLUTION: This new 3-aminomethylthiophene derivative is a compound of formula I [R1, R2 are each H, a halogen, hydroxy, nitro, a (halogen substituted) lower alkyl or the like; R3 is a lower alkyl; R4 to R7 are each H or a lower alkyl], e.g. N-(2-hydroxyethyl)-N-methyl-3-aminomethylthiophene. Further, the compound of formula I is obtained by reacting a thiophenecarboxyaldehyde derivative expressed by formula II with an ethanolamine derivative expressed by formula III in a solvent such as methanol in the presence of a reducing agent such as lithium aluminum hydride.

公开(公告)号：JPH0971562A

公开(公告)日：1997-03-18

申请号：JP18429196

申请日：1996-06-26

Applicant: GREEN CROSS CORP ,  TOSOH CORP

Inventor： ISHIDA NAOMICHI ,  AIDA MASAKI ,  YAMAURA YASUNARI ,  INOUE YOSHIHISA ,  NAKAMURA NORIFUMI ,  TOKUNAGA TAKUMI ,  HAGA KENICHI ,  TOKUHISA KENJI ,  KATSUURA KIMIO ,  HANAZAKI YASUAKI

IPC: C07D333/36 ,  A61K31/135 ,  A61K31/265 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C333/04 ,  C07C333/08 ,  C07D207/50 ,  C07D213/64 ,  C07D333/38 ,  C07D405/12 ,  C07D409/12

Abstract: PROBLEM TO BE SOLVED: To obtain a thiocarbamic acid derivative useful as an antihypercholesterolemia agent, an antihyperlipemia agent and an agent for treating and preventing arteriosclerosis and high in safety. SOLUTION: A thiocarbamic acid derivative of formula I m is 0,1; A is a group of formula II; R , R are each H, formyl, an alkyl; R is H, an acyl, etc.; R is phenyl, a six-membered heterocyclic group; R , R are each an alkyl, an alkoxy, etc.; Z is N, CH, etc.,}, e.g. 1-(3-aminophenoxy)-2-methoxy-3-(N- methyl-N-phenylamino)propane. The compound of formula I is obtained by reacting a halogenated thioformate of the formula: AOCSX (X is a halogen) with an amine of formula III.

公开(公告)号：JPH08301841A

公开(公告)日：1996-11-19

申请号：JP13612295

申请日：1995-05-10

Applicant: GREEN CROSS CORP ,  TOSOH CORP

Inventor： ISHIDA NAOMICHI ,  AIDA MASAKI ,  YAMAURA YASUNARI ,  INOUE YOSHIHISA ,  NAKAMURA NORIFUMI ,  KATSUURA KIMIO ,  TOKUHISA KENJI ,  TOKUNAGA TAKUMI ,  HANAZAKI YASUAKI

IPC: C12N9/99 ,  A61K31/16 ,  A61K31/17 ,  A61K31/265 ,  A61K31/27 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4433 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07C271/58 ,  C07C275/28 ,  C07C327/44 ,  C07C327/48 ,  C07C329/04 ,  C07C333/04 ,  C07C333/08 ,  C07C335/16 ,  C07D213/75 ,  C07D333/18 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

Abstract: PURPOSE: To obtain a new squalene-epoxydase activity inhibitor having high safety and excellent anticholesterol action and useful for treating and preventing hypercholesterolemia, hyperlipemia and arterial sclerosis. CONSTITUTION: This squalene-epoxydase inhibitor contains a compound of formula I [Q, V and W are each O, S, etc.; Z is CH or N; (m), (n), (p) and (g) are each 0 or 1; A is a group of formula II (R to R are H, a lower alkyl, an aralkyloxy, a halogen, hydroxyl group, etc.); R to R are each H, a lower alkyl, an alkylthio, a halogen, formyl, etc.,] or its pharmaceutical permissible salt as active ingredients. For example, O-p-t-buthylphenyl=N-m- tolylthiocarbamate is obtained by dropping acetonirile solution of p-t- butylphenylchlorothio-formate to acetonitrile solution of m-toluidine and potassium carbonate under ice cooling and reacting these components.

公开(公告)号：JPH08301826A

公开(公告)日：1996-11-19

申请号：JP13612195

申请日：1995-05-10

Applicant: GREEN CROSS CORP ,  TOSOH CORP

Inventor： ISHIDA NAOMICHI ,  AIDA MASAKI ,  YAMAURA YASUNARI ,  INOUE YOSHIHISA ,  NAKAMURA NORIFUMI ,  TOKUNAGA TAKUMI ,  HANAZAKI YASUAKI ,  KATSUURA KIMIO

IPC: C12N9/99 ,  A61K31/16 ,  A61K31/17 ,  A61K31/265 ,  A61K31/27 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4433 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C233/11 ,  C07C233/65 ,  C07C271/44 ,  C07C271/48 ,  C07C275/28 ,  C07C275/32 ,  C07C327/22 ,  C07C327/44 ,  C07C327/48 ,  C07C329/04 ,  C07C333/04 ,  C07C333/08 ,  C07C335/16 ,  C07D213/75 ,  C07D409/14

Abstract: PURPOSE: To produce a new compound, having high inhibiting activities against squalene epoxidase derived from mammals and useful for treating hypercholesterolemia, etc. CONSTITUTION: This compound is expressed by formula I [Q, V and W are each mutually independent O, S or the formula N-R (R is H, a lower alkyl, etc.), etc.; (l) and (n) are each 0 or 1; R is a lower alkyl, etc.; R is formula II (Z is the formula CH or N; R is a lower alkyl, etc.), except that R is a 1-4C alkyl, a halogen or a lower alkoxy when W an Q are each mutually independent O or S; V is the formula N-R ; (n) is 0; R is a lower alkyl, etc.; R is a lower alkyl], e.g. O-p-t-butylphenyl N-methyl-N-3- hydroxyphenylthiocarbamate. The compound of formula V is obtained by reacting a halogenoformate of formula III (W2 is O or S; X is Cl, Br, etc.) with an amine of formula IV.

公开(公告)号：JPH06306065A

公开(公告)日：1994-11-01

申请号：JP9425793

申请日：1993-04-21

Applicant: TOSOH CORP

Inventor： HANAZAKI YASUAKI ,  IDE TERUHIKO ,  FUJIWARA MASAHISA ,  WATANABE HIROYUKI ,  KATSUURA KIMIO

IPC: A01N43/832 ,  A01N43/82 ,  A61K31/41 ,  A61K31/433 ,  A61P31/04 ,  A61P31/10 ,  C07D285/10

Abstract: PURPOSE:To obtain the novel compound, excellent in antifungal activity and useful as a medical germicide. CONSTITUTION:The compound is expressed by formula I [X and Y are H, halogen, 1-6C alkyl, 1-4C alkoxy, nitro, trifluoromethyl, carboxyl or 1-4C alkoxycarbonyl; R is 1-6C alkyl), e.g. 2-methyl-4-phenoxy-1,2,5-thiadiazol-3(2H)- one. This compound expressed by formula I is obtained by reacting a compound expressed by formula II with an alkylating agent.