Takeda Pharmaceutical Company Limited

Mitsubishi Pharma Corporation

Takanobu Kuroita

Hiroki Sakamoto

Yasuhiro Imaeda

Hidekazu Tokuhara

Kouichi Iwanaga

Naohiro Taya

Minoru Sasaki

Hideyuki Igawa

Mami Ojima

Kouhei Asano

Akira Nishiyama

Tsuyoshi Maekawa

Yoshiyuki Fukase

Masanori Minoguchi

Koji Fuji

Masahiro Bougauchi

Shinkichi Suzuki

Keiji Kubo

Masaki Kawamura

Masakazu Fujio

Masatoshi Kiuchi

Michiko Tawada

Yoshihito Tanaka

Hidemitsu Higashi

Hideo Tomozane

Haruto Nakagawa

Yasunori Morio

Kouji Kanzaki

Shigeki Kuwahara

Shuuzou Takeda

Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.

Heterocyclic compound and use thereof

Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.

Compounds represented by the formulas (I) (II) wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like. 

A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.

Amide compounds and use of the same

A compound represented by the formula (I): wherein R1 is an oxo group, &#x2550;N&#x2014;R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, &#x2014;CO&#x2014;R8 or &#x2014;O&#x2014;R8', or a salt thereof. For example, the compound may be substituted pyrimidines and pharmaceutical compositions of the formula (I) where X=&#x2014;CR3; X1=&#x2014;CR2 or &#x2014;NR2; and X2=&#x2014;CR5 or &#x2014;NR5. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

Substituted pyrimidines and [1,2, 4] triazoles and the use thereof for treating prophylaxis, cardiovascular diseases, metabolic diseases and/or central nervous system diseases

The present invention relates to a compound represented by the formula (I) wherein Ris a group represented by the formula wherein R, R, R, R, R, Rand Rare each independently a hydrogen atom or a Calkyl, or a salt thereof. The compound of the present invention is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and metabolic diseases such as diabetes and the like.

Benzimidazole derivative and use as a II receptor antagonist

A compound represented by the formula (I):    

Heteromonocyclic compound or a salt thereof having strong antihypertensive action, insulin sensitizing activity and the like production thereof and use thereof for prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases

A thiazoline derivative represented by Formula (I): wherein R is a cyclic hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; X is a bond or a divalent chain hydrocarbon group which may be substituted; X' is a bond or &#x2014;N(R)&#x2014;; Y is a divalent hydrocarbon group which may be substituted; Y&#x2032; is a bond or &#x2014;C(&#x2550;O)&#x2014;; ring A is a nitrogen-containing heterocycle which may be substituted; Zand Zare each independently a bond or a divalent chain hydrocarbon group which may be substituted; Zis a bond or &#x2014;N(R)&#x2014;; and B is a group represented by the formula: which is useful as a therapeutic drug for thrombosis, is provided.

Thiazoline derivative and use of the same

The present invention relates to a phenoxypropylamine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof or a pharmaceutically acceptable salt thereof and hydrates thereof, which simultaneously show selective affinity for and antagonistic activity against 5-HTreceptor, as well as 5-HT reuptake inhibitory activity, and can be used as antidepressants quick in expressing an anti-depressive effect.

Phenoxypropylamine compounds

Benzimidazole derivative and use thereof

The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.

Benzylpiperidine compound

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Osaka, Japan

Takanobu Kuroita