Kyorin Pharmaceutical Co., Ltd.

Teijin Pharma Limited

Sagami Chemical Research Center

Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Yasumichi Fukuda

Yoshikazu Asahina

Masanori Yamamoto

Koji Murakami

Shiro Terashima

Shigeki Seto

Masanori Takadoi

Tomohiro Ide

Ayako Nakamura

Masahiro Nomura

Anna Katrin Szardenings

Kohei Ohata

Bei Li

Yasuo Oomori

Kyoko Okada

Kazuhiro Yumoto

Oana Cociorva

Kazuya Yokota

Shinji Kobayashi

Yasushi Kohno

Fumiyoshi Kobayashi

Hiroyuki Ebisu

Toshiyuki Matsui

Kanji Komatsu

Kenji Fujita

Futoshi Shiga

Masaya Takei

Hideyuki Fukuda

Taro Sato

Satoru Katayama

Taku Shibue

Milton L Hammond

Haruaki Kurasaki

Rumiko Shimazawa

Katrin Szardenings

A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein Rand Rare each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a Cto Calkyl group, a Cto Calkoxy group, a Cto Calkylsulfanyl group, a Cto Calkylsulfinyl group, a Cto Calkylsulfonyl group, or a Cto Calkoxy-Cto Calkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).

Cyclopentylacrylamide derivative

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

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. 

To provide a novel mutilin derivative having a substitution at the 14-position, which is a novel mutilin analogue exhibiting a potent and broad antimicrobial action against Gram-positive bacteria and Gram-negative bacteria including various drug-resistant bacteria, and which is expected to be useful as an agent for treating infectious diseases. A mutilin derivative represented by the following general formula (1): or a pharmaceutically acceptable addition salt thereof.

Mutilin derivative having heterocyclic aromatic ring carboxylic acid structure in substituent at 14-position

A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; Rand Rare each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C-Calkyl group, a C-Calkoxy group, a C-Calkylsulfanyl group, a C-Calkylsulfinyl group or a C-Calkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.

Glucokinase activator

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

Summary Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. Solving Means The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

Bicycloester derivative

A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, Rrepresents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C-Calkyl group, or a C-Calkoxy group, Rrepresents a C-Ccycloalkylsulfanyl group, a C-Ccycloalkylsulfinyl group, or a C-Ccycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).

Novel intermediates for the production of aminoacetyl pyrrolidine carbonitrile derivatives ensure the safe and efficient production of the compounds. Specifically, the present invention provides a sulfonyloxyacetyl pyrrolidine derivative, represented by the following formula: (Chemical Formula 1) (wherein R1 is a substituted or unsubstituted C-Calkyl group, a substituted or unsubstituted C-Ccycloalkyl group, a substituted or unsubstituted arylmethyl group, a substituted or unsubstituted aromatic hydrocarbon, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted aliphatic heterocyclic ring; R2 is CONHor CN; and X is CH, CHF or CF.)

Process for producing aminoacetyl pyrrolidine carbonitrile derivative and intermediate for production thereof

Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such asand other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

Cyclopropyl group substituted oxazolidinone antibiotics and derivatives thereof

Novel bicycloamide derivatives (general formula (1)) and pharmaceutically acceptable salts thereof effectively inhibit DPP-IV. The bicycloamide derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(4-carbamoylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

Bicycloamide derivative

A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor:  One example is (2S,4S)-1-[[N-(4-methylbicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile).

Bicyclo derivative

This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistantandspp.,spp. species, as well as acid-fast organisms such asand other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

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Tochigi, Japan

Yasumichi Fukuda