公开(公告)号：KR840001287B1

公开(公告)日：1984-09-07

申请号：KR840002710

申请日：1984-05-18

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： UEDA IKUO ,  NAGANO MASANOBU ,  KATO MASAYUKI

IPC: C07D239/86 ,  C07D487/04 ,  C07D487/14

公开(公告)号：KR840001315B1

公开(公告)日：1984-09-11

申请号：KR840002711

申请日：1984-05-18

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： UEDA IKUO ,  KATO MASAYUKI ,  NAGANO MASANOBU

IPC: C07D239/86 ,  C07D487/04 ,  C07D487/14

公开(公告)号：KR840001040B1

公开(公告)日：1984-07-26

申请号：KR840002712

申请日：1984-05-18

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： UEDA IKUO ,  NAGANO MASANOBU ,  KATO MASAYUKI

IPC: C07D239/86 ,  C07D487/04 ,  C07D487/14

公开(公告)号：JP2001220375A

公开(公告)日：2001-08-14

申请号：JP2000359201

申请日：2000-11-27

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： ITO KIYOTAKA ,  GLEN W SPEARS ,  YAMADA AKIRA ,  TOMIJIMA MASANORI ,  KATO MASAYUKI

IPC: C07D213/36 ,  A61K31/167 ,  A61K31/335 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4402 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07C257/18 ,  C07D209/42 ,  C07D209/88 ,  C07D209/94 ,  C07D313/08

Abstract: PROBLEM TO BE SOLVED: To obtain a new amide compound or its salt, in detail, a new amide compound having a pharmacological activity such as 5-hydroxytryptamine (5-HT) antagonism, etc., or its salt. SOLUTION: This compound is represented by general formula (I) R1-A- X-NHCO-R2 (I) (R1 is an aryl group which may contain a substituent group or a heterocyclic group which may contain a substituent group; R2 is a condensed phenyl group which may contain a substituent group, a phenyl group which may contain a substituent group or an indolin-1-yl group substituted with a lower alkylthio group and a trihalo (lower) alkyl group; A is a group of formula (II) or group (III) (R3, R4 and R5 are each a hydrogen atom or a lower alkyl group); X is a phenylene group or a lower alkylene group) or its salt.

公开(公告)号：JPH0262555B2

公开(公告)日：1990-12-26

申请号：JP16869080

申请日：1980-11-28

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： TAKATANI TAKAO ,  INOE ZENICHI ,  YASUDA NOBUSACHI ,  MURATA MASAYOSHI ,  UEDA IKUO ,  MATSUO MASAAKI ,  TSUJI KIRYO ,  KATO MASAYUKI

IPC: C07D501/18 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D209/48 ,  C07D257/04 ,  C07D277/20 ,  C07D295/13 ,  C07D295/205 ,  C07D501/36 ,  C07D501/57

公开(公告)号：JPH11130750A

公开(公告)日：1999-05-18

申请号：JP23496298

申请日：1998-08-05

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： ITO KIYOTAKA ,  GLEN W SPEARS ,  YAMANAKA TOSHIO ,  HARADA KEIKO ,  NODA YUKA ,  KATO MASAYUKI

IPC: C07D239/84 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/472 ,  A61K31/505 ,  A61K31/517 ,  A61P1/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D213/74 ,  C07D215/38 ,  C07D217/22 ,  C07D401/12 ,  C07D403/12

Abstract: PROBLEM TO BE SOLVED: To obtain a novel compound that is useful for treatment and prevention of central nervous system disorder as anxiety, depression, obsessive- compulsive neurosis and the like, withdrawal symptoms caused by drug abuse as cocaine, ethanol, nicotine or the like, schizophrenia or troubles relating to spinal trauma. SOLUTION: This novel compound is represented by formula I [R is quinolyl, quinazolinyl and the like; R is a group of the formula: -Y-R (R is phenyl or the like; Y is a lower alkylene) or its salts, typically 2,3- dihydro-1-[[3-[(isoquinoline-1-yl)aminomethyl]phenyl]carbamoyl]-indole. The compound of formula I is prepared by, for example, allowing a compound of formula II as 3-[(isoquinoline-1-yl)aminomethyl]aniline to react with a compound of formula III (X is a halogen) as 4-nitrophenyl chloroformate in a solvent as N,N-dimethylformamide followed by reaction of the product with 2,3- dihydroindole.

公开(公告)号：JPH10158241A

公开(公告)日：1998-06-16

申请号：JP33789697

申请日：1997-11-21

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： ITO KIYOTAKA ,  GLEN W SPEARS ,  YAMANAKA TOSHIO ,  HARADA KEIKO ,  NODA YUKA ,  KATO MASAYUKI

IPC: C07D487/04 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P43/00 ,  C07D209/08

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound having pharmacological activities such as a 5-HT antagonizing activity and useful for treating and preventing central nervous system diseases such as anxiety and Alzheimer's disease, etc. SOLUTION: A compound of formula I [R is a lower alkyl; R is a lower alkyl; R is H, etc.; R is phenyl, a heterocyclic group; X is methylene, iminomethylene; Y is a bond, carbonyl, etc.; (n) is 0, 1]. For example, 1-[[3-(N'- phenylamidino)phenyl]carbamoyl]-5methyl-2,3-dihydro-1H-pyrrolo [2,3-f]indole hydroiodide salt. The compound of formula I is produced by reacting a compound of formula II with a compound of the formula: R -Y-(NH)n -H in the presence of an acid such as an organic acid (e.g. formic acid) or an inorganic acid (e.g. HCl) in a solvent (e.g. water, CH3 OH) usually under cooling at room temperature or under heating.

公开(公告)号：JPH08283260A

公开(公告)日：1996-10-29

申请号：JP5644396

申请日：1996-03-13

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： KATO MASAYUKI ,  OKUBO MITSURU ,  SAKAI HIROYOSHI ,  TAKAHASHI FUMIE

IPC: C07D401/06 ,  A61K31/50 ,  A61P7/02 ,  A61P9/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C07D401/12

Abstract: PURPOSE: To produce the subject compound useful as an antagonistic agent for glycoproteins IIb/IIIb, an inhibitor of blood platelet aggregation and inhibitor of binding of a fibrinogen to blood platelets. CONSTITUTION: A compound of formula I [R is a (substituted)cyclo(lower) alkyl containing N; R is H or a lower alkyl; R is a (protected)carboxy; R is a (substituted)lower alkyl or an aryl; A is a (substituted)lower alkylene, a lower alkanyl-ylidene or a lower alkenylene; A is a lower alkylene; A is a (substituted)lower alkylene; X is O, S or NH; (m) and (n) are each a 0 or 1], e.g. N-[4,5-dihydro-6-methyl-2-[2-(piperidin-4-yl)ethyl]-3(2H)-oxopyridazin-4- yl]acetyl-β-alanine. Furthermore, this compound is obtained by reacting a compound of formula II or a reactive derivative at the carboxyl group or its salt with a compound of formula III or a reactive derivative at the carboxyl group or its salt.

公开(公告)号：JPH08152428A

公开(公告)日：1996-06-11

申请号：JP5976495

申请日：1995-02-22

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： KATO MASAYUKI ,  KITA YASUHIRO ,  NISHINO SHIGETAKA ,  HAMANO MITSUKO ,  TAKASUGI HISASHI ,  HIRASAWA YOSHIMI

IPC: G01N33/50 ,  C07C251/40 ,  C07D213/40 ,  C07D213/53 ,  C07D213/56 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D215/38 ,  C07D233/90 ,  C07D239/26 ,  C07D239/28 ,  C07D239/54 ,  C07D249/10 ,  C07D257/04 ,  C07D257/06 ,  C07D277/74 ,  C07D285/04 ,  C07D285/125 ,  C07D309/28 ,  C07D471/04

Abstract: PURPOSE: To obtain a standard reagent which immediately releases NO gas after being dissolved in water or a proper solvent by using a compound expressed by a specific formula or its salt as a main constituent. CONSTITUTION: A standard reagent uses a compound expressed by a formula I (R is hydrogen, a lower alkyl group etc., R and R are respectively hydrogen or lower alkyl groups, R and R are respectively hydrogen or form a single bond by mutual bounding, R is hydrogen or a lower alkyl group etc., R is hydrogen, hudroxyiminomethyl group, cyano group etc.) or its salt as main constituent. For example, a compound of formula II (R is hydrogen, a lower alkyl group etc., R , R , and R are respectively hydrogen or lower alkyl groups, and R is hydrogen etc.) is especially preferable. For example, methyl, ethyl etc., or 1-6C alkane residue in straight or branched chain are preferable as a lower alkyl group. These compounds are dissolved in a proper solvent such as water or dimethylsulfoxide and then immediately releases NO gas, thus easily drawing a calibration curve by the normal method.

公开(公告)号：JPH02117675A

公开(公告)日：1990-05-02

申请号：JP25298689

申请日：1989-09-27

Applicant: FUJISAWA PHARMACEUTICAL CO

Inventor： KATO MASAYUKI ,  ITO KIYOTAKA ,  TAKASUGI HISASHI

IPC: A61K31/435 ,  A61K31/44 ,  A61P1/00 ,  A61P1/04 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D471/04

Abstract: NEW MATERIAL:Compounds ot formula I [R is H, alkyl or alkenyl; R is H, alkyl or halogen; R is (substituted)imidazolyl or (substituted)pyridyl; R is R or hydroxyalkyl; R is H, OH or acyloxy; R and R are mutually bonded and form additional bond] and salts thereof. EXAMPLE:8,9-Dihydro-10-methyl-7-[(5-methyl-1H-imidazole-4-yl)methyl]py rido[1,2- a]indol-6(7H)-one. USE:A high-effect selective antagonist for 5-HT acceptor. Useful for remedy or protection of psychosis, central nervous system disease or aches such as headache or neuralgia. PREPARATION:A compound of formula II is, e.g., reacted with a compound of formula III or a salt thereof to obtain the objective compound of formula I where R is H and R is OH.