Kyorin Pharmaceutical Co., Ltd.

Kissei Pharmaceutical Co., Ltd.

Sagami Chemical Research Center

Shigeki Seto

Yasumichi Fukuda

Yasushi Kohno

Shigeru Izawa

Makoto Ikeda

Asao Tanioka

Masahiro Nomura

Anna Katrin Szardenings

Bei Li

Ayako Nakamura

Kazuhiro Yumoto

Kyoko Okada

Oana Cociorva

Kazuya Tatani

Atsushi Kondo

Tatsuhiro Kondo

Naohiro Kawamura

Shiro Terashima

Yasuo Oomori

Hiroyuki Ebisu

Katrin Szardenings

Yasmuchi Fukuda

Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases.

Spirocyclic aminoquinolones as GSK-3 inhibitors

The present invention provides a compound represented by the general formula (I) of the present invention, which has EPreceptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Yrepresents a Calkylene group or the like; Yrepresents a single bond or the like; Z represents &#x2014;C(&#x2550;O)&#x2014;NHSOR, an acidic 5-membered hetero ring group, or the like; Rrepresents a hydrogen atom or the like; Rrepresents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; Rrepresents a halogen atom, a Calkoxy group, or the like; Rrepresents a hydrogen atom, a halogen atom, or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a Calkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Indole derivative and pharmacologically acceptable salt thereof

The present invention provides a compound represented by the general formula (I) of the present invention, which has EPreceptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Yrepresents a Calkylene group; Yrepresents a single bond or the like; Rrepresents &#x2014;C(&#x2550;O)&#x2014;NH&#x2014;SOR, an acidic 5-membered hetero ring group, or the like; Rrepresents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; Rrepresents a halogen atom, a Calkoxy group, or the like; Rrepresents a hydrogen atom, a halogen atom, or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a Calkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Indole derivative, and pharmacologically acceptable salt thereof

Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases. In Formula (I): Xis O or NR; A is bond or substituted or unsubstituted C-Calkylene, wherein the substituents when present are selected from one to four Qgroups; where Qis alkyl or haloalkyl; p is 0 or 1; and q is an integer of 0 to 2. 

Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.

Aminoquinolones as GSK-3 inhibitors

A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; R is a hydrogen atom, a Cto Calkyl group, a Cto Calkylcarbonyl group, or a Cto Calkylsulfonyl group; m is 1 or 2; and n is 2 or 3.

Fused bicyclic pyrimidine derivatives

A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1):

Fused bicyclic pyridine derivatives as tachykinin receptor antagonists

A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof:

Fused bicyclic pyridine derivative as tachykinin receptor antagonist

A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1):wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; m is 1 or 2; and n is 2 or 3.

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Tochigi, Japan

Shigeki Seto