Seikagaku Corporation

Seikagaku Kogyo Kabushiki Kaisha

Fujirebio Kabushiki Kaisha

Tsuneo Koji

Nobuo Kobayashi

Hisatomo Kunii

Daisuke Morita

Akihiko Hosoda

Mizuho Ishikawa

Takashi Fujita

Tomofumi Nishimura

Masahiro Shibata

Akihiro Sekine

Masaharu Dozen

Mizuho Kataoka

Naoko Tanabe

Naoko Koji

The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an &#x3b1;-oxoacyl amino-caprolactam derivative that is represented by formula (I) (in the formula, X is &#x2014;O&#x2014; or &#x2014;N(R)&#x2014; and Rrepresents an alkoxycarbonyl group having 1-10 carbon atoms); and a bone resorption inhibitor containing the &#x3b1;-oxoacyl amino-caprolactam derivative.

Alpha-oxoacyl amino-caprolactam derivative

The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an &#x3b1;-oxoacyl amino-caprolactam that is represented by formula (I) (in formula (I), X represents N or CH, Y represents O or CH, and Z represents S or CH); and a bone resorption inhibitor containing the &#x3b1;-oxoacyl amino-caprolactam.

&#x3b1;-oxoacyl amino-caprolactam

The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an &#x3b1;-oxoacyl aminocaprolactam derivative that is represented by formula (I) (in the formula, X is &#x2014;O&#x2014; or &#x2014;N(R)&#x2014; and Rrepresents an alkoxycarbonyl group having 1-10 carbon atoms); and a bone resorption inhibitor containing the &#x3b1;-oxoacyl aminocaprolactam derivative.

&#x3b1;-oxoacyl amino-caprolactam derivative

Novel cycloalkane carboxamide derivatives having an action that selectively inhibits cathepsin K, and a production process thereof, are provided, wherein (wherein Rand Rrepresent (substituted) alkyl groups, (substituted) alkenyl groups, (substituted) alkynyl groups, (substituted) aromatic hydrocarbon groups or (substituted) heterocyclic groups, ring A represents an alkylidene group having 5 to 7 carbon atoms, and ring B represents a formyl group or a hydroxymethyl group).

Cycloalkane carboxamide derivatives and production process of same

Cycloalkylcarbonylamino acid ester derivatives, which are raw material intermediates for a novel cycloalkane carboxamide derivative having an action that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid ester derivative represented by formula (I), or a pharmaceutically acceptable salt thereof: (wherein, Rand Rrepresent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups, etc., Rrepresents an alkyl group having 1 to 6 carbon atoms, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).

Cycloalkylcarbonylamino acid ester derivative and process for producing the same

Novel raw material compounds are provided that are useful for producing novel cycloalkane carboxamide derivatives having cathepsin K inhibitory action. An oxazolone derivative represented by formula (I): [wherein, Rrepresents a substituted or unsubstituted alkyl group, substituted or unsubstituted alkenyl group, substituted or unsubstituted alkynyl group, substituted phenyl group, substituted or unsubstituted naphthyl group or substituted or unsubstituted heterocyclic group, and ring A represents a saturated cyclic alkylidene group having 6 to 7 carbon atoms].

Oxazolone derivative compounds having a 3-oxa-1-azaspiro[4.5] core

Cycloalkylcarbonylamino acid derivatives, which are raw material intermediates of a novel cycloalkane carboxamide derivative that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein, Rand Rrepresent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups or the like, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).

Cycloalkylcarbonylamino acid derivative and process for producing the same

The present invention is to provide manufacturing intermediates which can be led to useful &#x3b1;-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: 

Epoxycarboxamide compound, azide compound, and amino alcohol compound, and process for preparing &#x3b1;-keto amide compound using them

Epoxycarboxamide compound, azide compound, and amino alcohol compound, and process for preparing alpha-keto amide compound using them

A cyclic amide derivative of formula (I): ##STR1## wherein R.sup.1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sulfonamide group or a substituted amide group; the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms or a hetero-atom-containing saturated heterocyclic group with 3 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a hydrogen atom, a group represented by the general formula R.sup.4 O-- or a group represented by the general formula R.sup.5 (R.sup.6)N-- wherein R.sup.4 represents hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R.sup.5 and R.sup.6 may be the same or different and each represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group. The cyclic amide derivative of formula (I) have a strong and selective inhibitory action of a cathepsin K and a clinical efficacy when administered orally.

Growing community of inventors

Higashiyamato, Japan

Tsuneo Koji