Takeda Pharmaceutical Company Limited

Atsushi Hasuoka

Satoshi Yamamoto

Koji Ono

Masahiro Kajino

Haruyuki Nishida

Terufumi Takagi

Shinichi Imamura

Kazuhiro Miwa

Shigemitsu Matsumoto

Naoki Tarui

Yusuke Tominari

Taisuke Katoh

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 novel compound having a superior activity as an ERR-&#x3b1; modulator and useful as an agent for the prophylaxis or treatment of ERR-&#x3b1; associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

Nitrogen-containing heterocyclic compound

The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like. A proton pump inhibitor containing a compound represented by the formula (I) wherein ring A is a saturated or unsaturated 5- or 6-membered ring group optionally having, as a ring-constituting atom besides carbon atom, 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, ring-constituting atoms Xand Xare each a carbon atom or a nitrogen atom, a ring-constituting atom Xis a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, Ris an optionally substituted aryl group or an optionally substituted heteroaryl group, Ris an optionally substituted alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group, Ris an aminomethyl group optionally substituted by 1 or 2 lower alkyl groups, which is a substituent on a ring-constituting atom other than X, Xand X, and ring A optionally further has substituent(s) selected from a lower alkyl group, a halogen atom, a cyano group and an oxo group, or a salt thereof or a prodrug thereof.

Aryl- or heteroaryl-sulfonyl compounds as acid secretion inhibitors

A compound represented by the formula (I) wherein ring A is a 5- to 8-membered ring optionally having further substituent(s) other than R, Rand R,Ris an electron-withdrawing group,R, R, Rand Rare each independently a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom,Ris a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom,Ris a cyano group, a nitro group, an acyl group optionally having substituent(s), an optionally esterified or amidated carboxyl group or a hydrocarbon group optionally having substituent(s), or Rand Roptionally form, together with the carbon atom bonded thereto, a ring optionally having substituent(s), andRis a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, or a salt thereof has a superior action as an androgen receptor modulator, and is useful for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia, osteoporosis and the like.

Cyclic amine compound

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

A compound represented by the formula (I'): or a salt thereof, has a superior androgen modulating action, wherein R, R, R4 to R, Rand Rare defined in the claim.

Pyrrolidin-2-one derivatives as androgen receptor modulator

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

A compound represented by the formula (I) each symbol of which is defined in the specification, or a salt thereof which has a superior androgen receptor regulating activity.

The present invention provides an aryl- or heteroaryl compound represented by the formula (Ia) or (Ib) wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. The compound has superior acid secretion inhibitory action, an antiulcer activity and the like.

Aryl-or heteroaryl-sulfonyl compounds as acid secretion inhibitors

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

The present invention relates to pharmaceutical agents which are agents for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; the pharmaceutical agents frailty suppressants, muscle strength enhancers, muscle increasing agents, cachexia suppressants, body weight decrease suppressants, agents for the prophylaxis or treatment of prostate hypertrophy, amyotrophy or muscle loss caused by a disease or an agent for reducing the prostate weight. The present invention also relates to methods for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis in a mammal, which comprises administering an effective amount of the pharmaceutical agents of the present invention or a prodrug thereof; use of the pharmaceutical agents of the present invention or a prodrug thereof for the production of an agent for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; and the like.

Growing community of inventors

Osaka, Japan

Atsushi Hasuoka