Astellas Pharma Gmbh

Takeda Pharmaceutical Company Limited

Kotobuki Pharmaceutical Co Ltd

Jiro Fujiyasu

Fukushi Hirayama

Yuji Koga

Susumu Yamaki

Takashi Kamikubo

Hiroyuki Moritomo

Norio Seki

Jun Takasaki

Toshihiro Watanabe

Takao Okuda

Susumu Watanuki

Tomoyoshi Imaizumi

Satoshi Sasamura

Michihito Kageyama

Tomohki Satou

Toshio Uemura

Daisuke Suzuki

Hiroshi Tomiyama

Kenji Negoro

Kazuhiko Ohne

Ken-Ichi Suzuki

Masahiro Neya

Norio Asai

Daisuke Kaga

Kousei Yoshihara

Satoshi Hayashibe

Masamichi Okada

Takeshi Hondo

Toru Asano

Yasuharu Urano

Yoshinori Iwai

Keisuke Matsuura

Makoto Oku

Daisuke Sasuga

Motoharu Sonegawa

Hirotsune Itahana

Kazuo Tokuzaki

Osamu Kaneko

Yukinori Nagakura

Kazumi Kikuchi

Takashi Toya

Yuka Koike

[Problem] To provide a compound which is useful as an agent for preventing and/or treating kidney diseases. [Means for Solution] The present inventors have studied compounds having a trypsin inhibitory activity, and have confirmed that a guanidinobenzoic acid ester compound has a trypsin inhibitory activity, thereby completing the present invention. The guanidinobenzoic acid ester compound of the present invention can be used as an agent for preventing and/or treating kidney diseases (for example, chronic kidney disease, acute glomerulonephritis, acute kidney injury, and the like) as an agent which will substitute low-protein diet therapy, and/or as an agent for preventing and/or treating trypsin-related diseases (for example, chronic pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like).

Guanidinobenzoic acid ester compound

[Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.

Guanidinobenzoic acid compound

Compounds of formula (I) defined herein exhibit VAP-1 inhibitory activity, and as a result, are useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention.

Glycine compound

Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; &#x2014;N(R)C(O)-lower alkylene-COR, lower alkylene-COR, lower alkenylene-COR, &#x2014;O-lower alkylene-COR, &#x2014;O-(lower alkylene which may be substituted with &#x2014;COR)-aryl or &#x2014;O-lower alkenylene-COR(wherein Ris H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.

Quinolone derivative or pharmaceutically acceptable salt thereof

Provided are quinolone derivatives having a lower alkyl or cycloalkyl at the 1-position; &#x2014;N(R)C(O)-lower alkylene-COR, lower alkylene-COR, lower alkenylene-COR, &#x2014;O-lower alkylene-COR, &#x2014;O-(lower alkylene which may be substituted with &#x2014;COR)-aryl or &#x2014;O-lower alkenylene-COR(wherein Ris H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof. Pharmaceutical composition containing the quinolone derivatives and methods of using the compositions are provided.

The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.

Nitrogen&#x2014;containing heterocyclic derivatives having 2,6-disubstituted styryl

Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli. Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.

Benzene derivative or salt thereof

This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R: an oxygen-containing saturated hetero ring or the like, Alk: a lower alkylene, m: 0 or 1, Alk: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR, R: H or the like, and R, R, R, Rand R: the same or different from one another and each represents H or the like. Provided that Rdoes not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, Rrepresents a group other than Me when m is 1, Ris OH or OMe and Alkis a Calkylene, and further 1) when X is a bond, n is 1 and Ris H, or 2) when X is a bond, n is 0 and Ris cyclohexane.)

Aminomethyl-substituted thiazolobenzimidazole compounds

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Tokyo, Japan

Jiro Fujiyasu