Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Naoki Tarui

Yu Momose

Ken-ichi Naruo

Junji Matsui

Hirokazu Matsumoto

Takayuki Doi

Tetsuo Miwa

Yoshinori Ikeura

Chieko Kitada

Masaaki Mori

Junya Shirai

Hideaki Natsugari

Hiroyuki Watanabe

Tetsuya Ohtaki

Hiroshi Banno

Taiji Asami

Mitsuo Yamamoto

Tsuneo Kanamaru

Kazuo Nakahama

Atsushi Hasuoka

Masahiro Kajino

Osamu Uchikawa

Terufumi Takagi

Yasuhiko Kawano

Kazuyoshi Aso

Toshiaki Nagata

Takenori Ishimaru

Shiro Takekawa

Osamu Kurasawa

Masakuni Kori

Motowo Izawa

Yutaka Nakayama

Chiharu Kimura

Tadatoshi Hashimoto

Nobuhiro Fujii

Tatsumi Matsumoto

Kohji Fukatsu

Kiyoharu Matsumoto

Naoko Nishizawa

Yoichi Nagano

Takashi Santo

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 metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action.

Metastin derivatives and use thereof

The present invention provides a compound represented by the formula: 

Bicyclic piperazine compound having TGR23 antagonistic activity

The present invention provides a compound represented by the formula:  wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, Ris a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, Ris not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

Piperidine derivative, process for producing the same, and use

A novel biphenyl compound having GPR 14 antagonistic activity. It is a compound represented by the formula (I): wherein Rrepresents hydrogen, etc.; X represents 1 to 12 spacers; A represents amino, etc., Rand Reach represents a hydrocarbon group, etc.; and rings B and C each represents an optionally further substituted benzene ring, or a salt thereof.

Biphenyl compound

Compounds of the formula wherein R, R, R, R, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.

Pyrimidine 5-carboxamide compounds, process for producing the same and use thereof

A compound having a partial structure represented by Formula:or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic agent against inflammatory diseases, for example, bronchial asthma, chronic obstructive pulmonary disease (COPD), rheumatoid arthritis, autoimmune disease, diabetes and the like.

Furoisoquinoline derivatives, process for producing the same and use thereof

Apoptosis inhibitor

An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: --CO--, --CH(OH)-- or --NR.sup.3 -- where R.sup.3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R.sup.1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R.sup.1 ; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.

Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C&lt;, --CO--N&lt; or --CS--N&lt; as the partial structure --X . . . Y&lt;; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has anexcellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Cyclic compounds, their prudiction and use

A process for producing an optically active form of a compound of formula (I) ##STR1## wherein R.sub.1 represents hydrogen or a hydrocarbon group that may be substituted; R.sub.2 and R.sub.3 independently represent hydrogen, a hydrocarbon group that may be substituted, or a heteroaromatic group that may be substituted; X' represents a substituent comprising an esterified carboxyl group or an acylated hydroxyl group; ring A represents a benzene ring that may be substituted or a heteroaromatic ring that may be substituted; ring J' represents a 7- or 8-membered heterocyclic ring containing at most 3 hetero-atoms as ring-constituent members, which may have a further substituent or substituents in addition to R.sub.1, R.sub.2, R.sub.3 and X', and C* denotes a chiral carbon atom or a salt thereof, which comprises subjecting the racemic compound of the formula (I) or a salt thereof, or alternatively a racemic starting compound for synthesizing the compound of the formula (I) to enzymatically enantioselective hydrolysis to provide an optically active form thereof.

Process for enantioselective hydrolysis of

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Nara, Japan

Naoki Tarui