Takeda Pharmaceutical Company Limited

Masahiro Kajino

Atsushi Hasuoka

Haruyuki Nishida

Haruhide Kimura

Yutaka Nakayama

Yasuhiko Kawano

Terufumi Takagi

Taisuke Tawaraishi

Akira Kawada

Koji Ono

Yasuyoshi Arikawa

Naoki Tarui

Keizo Hirase

A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, Ris an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R, Rand Rare the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, Rand Rare the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug thereof is provided.

Proton pump inhibitors

The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity, which is represented by the formula (I) wherein Ris an optionally substituted cyclic group, Ris a substituent, Ris an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, Rand Rare each a hydrogen atom, an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, Rand Rare each a hydrogen atom or an alkyl group, and n is an integer of 0-3, or a salt thereof.

Pyrrole compounds

The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein Ris a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), Ris an optionally substituted Caryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, Rand Rare each a hydrogen atom, or one of Rand Ris a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and Ris an alkyl group or a salt thereof. 

1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors

The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein Ris a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), Ris an optionally substituted Caryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, Rand Rare each a hydrogen atom, or one of Rand Ris a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and Ris an alkyl group or a salt thereof.

Acid secretion inhibitor

The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein Ris a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), Ris an optionally substituted Caryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, Rand Rare each a hydrogen atom, or one of Rand Ris a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and Ris an alkyl group or a salt thereof. 

1-heterocyclylsulfonyl, 3-aminomethyl, 5-(hetero-)aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors

1-heterocyclylsulfonyl, 3-aminomethyl, 5-(hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors

1-heterocyclylsulfonyl, 2-aminomethyl, 5-(hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors

The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Ris a hydrogen atom and the like; Ris a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; Ris unsubstituted (i.e., absence), a hydrogen atom and the like; Rand Rare the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; Ris (cyclic group optionally having substituent(s))-carbonyl, and the like; R, R, Rand Rare the same or different and each is a hydrogen atom, halogen and the like; or Rand R, Rand R, and Rand Rmay form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;--- represents unsubstituted (i.e., absence) or a single bond; andrepresents a single bond or a double bond, or a salt thereof, and the like.

Fused quinoline derivative and use thereof

The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Ris a hydrogen atom and the like; Ris a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; Ris unsubstituted (i.e., absence), a hydrogen atom and the like; Rand Rare the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; Ris (cyclic group optionally having substituent(s))-carbonyl, and the like; R, R, Rand Rare the same or different and each is a hydrogen atom, halogen and the like; or Rand R, Rand R, and Rand Rmay form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;&#x2003;represents unsubstituted (i.e., absence) or a single bond; and&#x2003;represents a single bond or a double bond, or a salt thereof, and the like.

This invention provides a compound represented by the formula (I): wherein Ris a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents;Ris pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents;n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.

1,3-benzothiazinone derivatives and use thereof

As prophylactic and/or therapeutic agents for cardiovascular diseases, bone or joint diseases, infectious diseases, inflammatory diseases, kidney diseases, etc. having safe and excellent effects of cell death inhibition, MIF binding, etc., there are provided compounds represented by formula: [wherein, Rrepresents a halogen atom, etc., Rrepresents a group represented by formula: (wherein, Rrepresents hydrogen atom, an optionally substituted alkoxy, etc., Rrepresents hydrogen atom, bromine atom, cyano, etc., Rrepresents hydrogen atom, hydroxy, etc., Rrepresents hydrogen atom, etc., Rrepresents hydrogen atom, etc.) etc., and n represents an integer of 0 to 4] or salts thereof.

1,3-Benzothiazinone derivatives, process for producing the same use thereof

The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Ris a hydrogen atom and the like; Ris a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; Ris unsubstituted (i.e., absence), a hydrogen atom and the like; Rand Rare the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; Ris (cyclic group optionally having substituent(s))-carbonyl, and the like; R, R, Rand Rare the same or different and each is a hydrogen atom, halogen and the like; or Rand R, Rand R, and Rand Rmay form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;

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Osaka, Japan

Masahiro Kajino