Banyu Pharmaceutical Co. Ltd

Banyu Pharmaceutical Coaltd

Kazuhito Noguchi

Norikazu Otake

Tomoshige Numazawa

Yoshio Ogino

Kenji Matsuda

Toshifumi Kimura

Hideki Kurihara

Toru Fujikawa

Akira Naya

Yufu Sagara

Minaho Uchiyama

Takehiro Fukami

Kenji Matsuyama

Morihiro Mitsuya

Kiyofumi Ishikawa

Toshiaki Mase

Takashi Hayama

Mitsuo Yano

Takeru Yamakawa

Kenji Ohwaki

Makoto Ando

Kensuke Kobayashi

Toshihiko Saeki

Yuki Iwahori

Seita Koito

Mitsuru Miyaji

This invention relates to compounds which exhibit selective muscarinic Mreceptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I);  [in which A signifies a group expressed by a formula (a) or (b); Ar signifies optionally substituted aryl or heteroaryl; Band Bsignify aliphatic hydrocarbon; Rsignifies fluorine-substituted cycloalkyl; R, Rand Rsignify lower alkyl, single bond or alkylene bonded to B, or Rand Rare united to signify alkylene; Rand Rsignify hydrogen, lower alkyl, or a single bond or alkylene bonded to B; Rsignifies hydrogen, lower alkyl or a group expressed as &#x2014;N(R)R; and Xsignifies an anion].

Ester derivatives

This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [a] or [b]  The compounds of the invention exhibit selective antagonism to muscarinic Mreceptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

Amide derivatives

This invention relates to compounds which exhibit selective muscarinic Mreceptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I);  Ar signifies optionally substituted aryl or heteroaryl; Band Bsignify aliphatic hydrocarbon; Rsignifies fluorine-substituted cycloalkyl; R, Rand Rsignify lower alkyl, single bond or alkylene bonded to B, or Rand Rare united to signify alkylene; Rand Rsignify hydrogen, lower alkyl, or a single bond or alkylene bonded to B; Rsignifies hydrogen, lower alkyl or a group expressed as &#x2014;N(R)R; and Xsignifies an anion].

This invention relates to compounds which exhibit selective muscarinic Mreceptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I);

Substituted imidazolidinone derivatives

Substituted piperidine derivatives as muscarinic M.sub.3 receptor

There are provided novel aminophosphonic acid derivatives of the general formula [I]: ##STR1## wherein n is an integer of 2 or 3; R.sup.1 is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R.sup.2 is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a .beta.-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or N.sup..omega. -nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.

Aminophosponic acid derivative

Growing community of inventors

Tsukuba, Japan

Kazuhito Noguchi