Ono Pharmaceutical Co., Ltd.

Ono Pharmaceuticals Co., Ltd.

Manabu Fujita

Jun Takeuchi

Yoshisuke Nakayama

Satoshi Itadani

Shinya Takahashi

Tadashi Tatsumi

Kazuyuki Ohmoto

Shizuka Ono

Takahiro Nekado

Junya Ueda

The present invention provides type C crystal of compound I, type B crystal of compound II, or type C crystal of compound III set forth in this specification.

Crystalline forms of 4, 4'-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl) butoxy] phenyl} ethynyl)-2-methyl-1H-indole-1,3-diyl] dibutanoic acid, 4,4&#x2032;-[2-methyl-7-({4-[4-(pentafluorophenyl) butoxy] phenyl} ethynyl)-1H-indole-1, 3-diyl] dibutanoic acid, and 4,4&#x2032;-[4-fluoro-2-methyl-7-({4-[4-(2, 3, 4, 6-tetrafluorophenyl) butoxy] phenyl} ethynyl)-1H-indole-1, 3-diyl] dibutanoic acid

The present invention relates to a compound of formula (I) (wherein all symbols have the same meanings as described hereinbefore). The compound antagonizes cysLTand therefore, it is useful as an agent for the prevention and/or treatment of respiratory diseases such as bronchial asthma, bronchial asthma, chronic obstructive pulmonary disease, pneumonectasia, chronic bronchitis, pneumonia (e.g. interstitial pneumonitis etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), and the like, or as an expectorant or antitussives.

Substituted indole derivatives for the treatment of respiratory diseases

As a compound having a potent oral activity and a long-lasting cysLT/cysLTreceptor antagonistic activity, the compound of the formula (I): which exhibits potent antagonistic activity against the cysLT/cysLTreceptor, and have long-lasting effects even in case of oral administration, and therefore is useful as an oral agent for preventing and/or treating a variety of diseases, for example, respiratory disease (for example, asthma (bronchial asthma, etc.), chronic obstructive pulmonary disease (COPD), pulmonary emphysema, chronic bronchitis, pneumonia (interstitial pneumonia, etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), apnea syndrome, allergic rhinitis, sinusitis (acute sinusitis, chronic sinusitis, etc.), pulmonary fibrosis, coughing (chronic coughing, etc.), and the like) was developed.

Ethynylindole compounds

Carboxylic acid derived benzoxazines as agents for the treatment of respiratory diseases

The present invention relates to a compound represented by the formula (I), 

Indole compound and use thereof

Growing community of inventors

Mishima-gun, Japan

Manabu Fujita