Astellas Pharma Gmbh

Yamanouchi Pharmaceutical Company Ltd.

Rational Drug Design Laboratories

Toru Kontani

Wataru Hamaguchi

Hiroshi Suzuki

Junji Miyata

Hiroshi Nagata

Akio Kamikawa

Tomoaki Kawano

Kenji Sudo

Koji Kato

Noriyuki Kawano

Kunihiro Niigata

Takayuki Suzuki

Kazuhiro Yokoyama

Tatsuya Maruyama

Kenichi Onda

Naoyuki Masuda

Tadashi Terasaka

Hisao Hamaguchi

Yuji Matsushima

Shinya Nagashima

Shunji Kageyama

Takumi Takahashi

Eiichi Nakai

Kyoichi Maeno

Yoji Miyazaki

Akiyoshi Shimaya

Reiko Koike

Hiroshi Inami

Osamu Noshiro

Takahiro Miyazaki

Tadatsura Koshika

Jun Irie

[PROBLEMS] Provided is a compound which has an antagonistic action on a muscarinic Mreceptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [MEANS For SOLVING PROBLEMS] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic Mreceptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic Mreceptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic Mreceptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

Aza-bridged-ring compound

To provide a compound which has an excellent activity to modulate the functions of CCR4 or TARC and/or MDC and can be used for the prevention and/or treatment of various inflammatory diseases, allergic diseases, autoimmune diseases and the like. An acylaminopiperidine compound represented by the formula (I) or a pharmaceutically acceptable salt thereof. [Symbols in the formula represent the following meanings; A: a single bond or C-Calkylene, R: phenyl which may be substituted, etc., R: &#x2014;H or C-Calkyl, R: &#x2014;H, C-Calkyl or C-Ccycloalkyl, R: pyrrolidin-2-yl which may be substituted, etc., and D: benzene ring or pyrazole ring].

Acylaminopiperidine compound

There is provided a pharmaceutical drug, particularly a novel compound useful for prophylaxis or a therapeutic treatment of various diseases involving infections with viruses of the herpesvirus family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. An N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative, of which phenyl group is substituted at position 4 with a specific 5- or 6-membered heteroaryl group, and a salt thereof have an effective anti-virus activity, and the oral administration thereof at a low dose enabled the therapeutic treatment of the above diseases.

Amide derivative

The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.

A pharmaceutical drug, particularly a novel compound useful for the prophylaxis or therapeutic treatment of various diseases involving infections with viruses of the Herpesviridae family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. N-{2-[(4-Substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative where the phenyl group is substituted at position 4 with a specific five-membered or 6-membered heteroaryl group, has such great anti-virus activity that the oral dosing thereof at a low dose enabled the therapeutic treatment of the diseases.

Tetrahydro-2H-thiopyran-4-carboxamide derivative

Bisoxadiazolidine derivative

Growing community of inventors

Tokyo, Japan

Toru Kontani