公开(公告)号：JP2645225B2

公开(公告)日：1997-08-25

申请号：JP24145694

申请日：1994-10-05

申请人： FUAIZAA INC

发明人： ITO FUMITAKA ,  KONDO YOJI ,  SHIMADA KAORU ,  NAKANE MASAMI ,  JON ADAMUSU RO ZA SAADO ,  TERII JEI ROOSEN ,  BINGUEI YANGU

IPC分类号： C07D453/02 ,  A01N43/90 ,  A61K20060101 ,  A61K31/395 ,  A61K31/435 ,  A61K31/439 ,  A61K31/44 ,  A61K31/445 ,  A61P1/00 ,  A61P1/16 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D453/00 ,  C07D453/04 ,  C07D471/10

摘要： PCT No. PCT/US92/03317 Sec. 371 Date May 23, 1994 Sec. 102(e) Date May 23, 1994 PCT Filed Apr. 28, 1992 PCT Pub. No. WO92/21677 PCT Pub. Date Dec. 10, 1992Compounds of the formula I wherein R1 is methoxy and R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

公开(公告)号：JPH07285965A

公开(公告)日：1995-10-31

申请号：JP24145694

申请日：1994-10-05

申请人： PFIZER

发明人： ITO FUMITAKA ,  KONDO YOJI ,  SHIMADA KAORU ,  NAKANE MASAMI ,  JIYON ADAMUSU ROU ZA SAADO ,  TERII JIEI ROOSEN ,  BINGUUEI YANGU

IPC分类号： C07D453/02 ,  A01N43/90 ,  A61K20060101 ,  A61K31/395 ,  A61K31/435 ,  A61K31/439 ,  A61K31/44 ,  A61K31/445 ,  A61P1/00 ,  A61P1/16 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D453/00 ,  C07D453/04 ,  C07D471/10

摘要： PCT No. PCT/US92/03317 Sec. 371 Date May 23, 1994 Sec. 102(e) Date May 23, 1994 PCT Filed Apr. 28, 1992 PCT Pub. No. WO92/21677 PCT Pub. Date Dec. 10, 1992Compounds of the formula I wherein R1 is methoxy and R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

公开(公告)号：JPH06500344A

公开(公告)日：1994-01-13

申请号：JP50013693

申请日：1992-05-08

IPC分类号： C07D317/20 ,  C07B61/00 ,  C07C29/04 ,  C07C29/48 ,  C07C31/20 ,  C07C33/26 ,  C07C67/31 ,  C07C69/675 ,  C07C69/732 ,  C07D317/30 ,  C07D453/04

公开(公告)号：JPH04295455A

公开(公告)日：1992-10-20

申请号：JP8483291

申请日：1991-03-25

申请人： LION CORP

发明人： TSUCHIYA YOSHIKAZU ,  KOBAYASHI OSAMU ,  MUKOYAMA MITSUAKI

IPC分类号： B01J31/02 ,  B01J31/18 ,  C07B61/00 ,  C07C253/00 ,  C07C255/12 ,  C07C255/31 ,  C07C255/36 ,  C07C255/42 ,  C07D453/04

摘要： PURPOSE:To obtain the objective compound in high yield and readily in production of a cyano compound useful as a raw material especially for medicines, agricultural chemicals and liquid crystal substance by cyanating a nucleophilic reaction accepting compound with a trisubstituted silylanilide by using a specific catalyst. CONSTITUTION:In cyanating a nucleophilic reaction accepting compound such as carbonyl compound, e.g. aldehyde or ketone, imine compound or nitroolefin compound, preferably aldehyde with a trisubstituted silylanilide, a Lewis base such as organic amine compound, organic phosphorus compound, organic arsenic compound or organic antimony compound, preferably cinchonine or a derivative thereof, especially a cinchonine derivative shown by the formula (Tb is trifluoromethanesulfonic acid residue) as an asymmetric synthetic catalyst to improve yield, especially optical yield of the objective compound. The catalyst for asymmetric synthesis is readily obtainable and more stably and inexpensively supplied than existing catalysts for asymmetric synthesis.

公开(公告)号：JPH03279372A

公开(公告)日：1991-12-10

申请号：JP17572990

申请日：1990-07-02

申请人： YOSHITOMI PHARMACEUTICAL

发明人： KAWAKITA TAKESHI ,  KUROITA TAKANOBU ,  FUKUDA TAKEMI ,  IKEZAWA RYUHEI

IPC分类号： C07D279/16 ,  A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61K31/5415 ,  A61P1/00 ,  A61P25/00 ,  C07D265/36 ,  C07D413/12 ,  C07D417/06 ,  C07D451/04 ,  C07D451/12 ,  C07D451/14 ,  C07D453/04 ,  C07D473/00 ,  C07D475/00

摘要： NEW MATERIAL:The compound of formula I [R to R are H, alkyl, phenyl, heteroaryl, etc.; R is H, alkyl, alkanoyl, etc.; R to R are H, halogen, alkyl, etc.; X is O or S; Y is O or N-R (R is H or alkyl); R is group of formula II (m is 0 or 1; n is 0-2), etc.], its geometrical isomer, optical isomer and salt. EXAMPLE:6-Chloro-4-methyl-N-(3-quinuclidinyl)-3,4-dihydro-2H-1,4-benzo xazine-8- carboxamide. USE:The compound exhibits antagonistic action against 5-HT3 receptor and is useful for the remedy of diseases of neutral nervous system and gastrointestinal diseases. PREPARATION:The compound of formula I can be produced by reacting a compound of formula III or its reactive derivative with a compound of formula R -YH in the presence of a condensation agent (e.g. dicyclohexylcarbodiimide) in an inert solvent under cooling, at room temperature or under heating.

公开(公告)号：JPS6344755B2

公开(公告)日：1988-09-06

申请号：JP21167483

申请日：1983-11-10

申请人： PFIZER

发明人： CUE BERKELEY WENDELL JR ,  HAMMEN PHILIP DIETRICH ,  MASSETT STEPHEN SARGENT ,  MOORE BERNARD SHIELDS ,  SYSKO ROBERT JOHN

IPC分类号： C07C67/00 ,  C07C209/00 ,  C07C211/25 ,  C07D311/22 ,  C07D311/68 ,  C07D453/04 ,  C07D491/10 ,  C07D491/107

公开(公告)号：JPS63211282A

公开(公告)日：1988-09-02

申请号：JP1677488

申请日：1988-01-27

申请人： PFIZER

发明人： BAAKUREI UENDERU KIYUU JIYUNIA ,  FUIRITSUPU DEIITORITSUKU HAMUM ,  SUTEIIBUN SAAJIENTO MASETSUTO ,  BAANAADO SHIIRUZU MUUA ,  ROBAATO JIYON SHISUKO

IPC分类号： C07C67/00 ,  C07C209/00 ,  C07C211/25 ,  C07D311/22 ,  C07D311/68 ,  C07D453/04 ,  C07D491/10 ,  C07D491/107

公开(公告)号：JPS63211281A

公开(公告)日：1988-09-02

申请号：JP1677288

申请日：1988-01-27

申请人： PFIZER

发明人： BAAKUREI UENDERU KIYUU JIYUNIA ,  FUIRITSUPU DEIITORITSUKU HAMUM ,  SUTEIIBUN SAAJIENTO MASETSUTO ,  BAANAADO SHIIRUZU MUUA ,  ROBAATO JIYON SHISUKO

IPC分类号： C07C67/00 ,  C07C209/00 ,  C07C211/25 ,  C07D311/22 ,  C07D311/68 ,  C07D453/04 ,  C07D491/10 ,  C07D491/107

公开(公告)号：JPS6210640B2

公开(公告)日：1987-03-07

申请号：JP13965576

申请日：1976-11-22

申请人： MERCK & CO INC

发明人： JIIN ESU KEEHAN ,  FUREDERITSUKU EMU KEEHAN ,  EDOWAADO OO SUTAPUREI ,  SEBASUCHIAN ERUNANDESU

IPC分类号： C07D477/00 ,  A61K20060101 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61K35/74 ,  A61P31/04 ,  C07D205/00 ,  C07D207/00 ,  C07D453/04 ,  C07D473/08 ,  C07D487/04 ,  C07D489/04 ,  C07G11/00 ,  C12P1/06 ,  C12P17/10 ,  C12P17/18 ,  C12R1/465

摘要： The microorganism Streptomyces cattleya, preferably the strain NRRL 8057, is cultivated under submerged aerobic conditions in an aqueous nutrient medium containing assimilable C and N sources as well as inorganic salts. N-Acetylthienamycin is obtained. Non-toxic, pharmaceutically acceptable salts of N-acetylthienamycin can be obtained by reaction with inorganic or organic bases. N-acetylthienamycin and its salts show remarkable antibiotic properties and are active against a wide range of pathogens as well as against resistant strains of particular microorganisms. The antibiotic is active against Gram-positive and -negative bacteria and is suitable for use in human and veterinary medicine and as antibacterial agent for commercial and industrial purposes.

公开(公告)号：JPS6112689A

公开(公告)日：1986-01-21

申请号：JP13097585

申请日：1985-06-18

申请人： Ici Ltd

发明人： DEBUITSUDO ROBAATO BURITSUTEIN

IPC分类号： A61K31/40 ,  A61P3/08 ,  A61P3/10 ,  C07D209/34 ,  C07D209/38 ,  C07D453/04 ,  C07D487/10 ,  C12N9/99

CPC分类号： C07D487/10 ,  C07D209/34 ,  C07D209/38 ,  C07D453/04