Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Canon Kabushiki Kaisha

Rdiscovery, LLC

Akio Ojida

Akihiro Tasaka

Masami Kusaka

Tomohiro Kaku

Toru Yamano

Naohiro Taya

Masuo Yamaoka

Tetsuya Yano

Takashi Sakamoto

Kimihiro Yoshimura

Isao Aoki

Fumio Yamauchi

Takenori Hitaka

Nobuyuki Matsunaga

Mari Adachi

Itaru Hamachi

Motohiro Nishida

Naoya Shindo

Akiyuki Nishimura

Masaaki Inoue

Compounds represented by formula (I) below and pharmacologically acceptable salts thereof and solvates of them; pharmaceutical compositions and dynamin-related protein 1 (Drp1)-filamin complex formation inhibitors containing them; and uses of the compounds, salts, solvates, pharmaceutical compositions, and (Drp1)-filamin complex formation inhibitors for use as a prophylactic or therapeutic agent.

Drp1-filamin complex formation inhibitors

A compound which captures a multisite phosphorylated peptide or protein specifically to a phosphorylation site and a method for detecting the peptide or protein using the compound. Particularly, a compound which specifically detects an excessively phosphorylated tau protein observed in the brain affected by Alzheimer's disease and a method for diagnosing Alzheimer's disease in vitro or in vivo using the compound are provided. By bringing a metal complex compound having two dipicolylamine (Dpa) moieties and a spacer including a chromogenic or luminescent functional or atom group into contact with a multisite phosphorylated peptide or protein, the compound recognizes the distance between phosphate groups and specifically binds to the peptide or protein, and a multisite phosphorylated peptide or protein or kinase activity is optically detected by measuring the change, or a multisite phosphorylated peptide or protein or kinase activity is imaged by an optical imaging method applying the change in luminescence.

Multisite phosphorylated peptide (protein) recognizing compound and detection method, imaging method, alzheimer's disease diagnosing method and reagent kit using the same

The present invention provides a method for producing an optically active &#x3b2;-hydroxy ester compound represented by the general formula: wherein wherein the ring may be substituted and the like, wherein Rand Rare as defined above with a compound represented by the general formula: wherein R, Rand Rare as defined above, and X is a halogen atom.

Method for producing optically active compound

The present invention provides a method for producing an optically active &#x3b2;-hydroxy ester compound represented by the general formula: wherein Rrepresents an optionally substituted hydrocarbon group and the like, Rrepresents a nitrogen-containing heterocyclic group different from R, which is represented by the general formula: wherein the ring may be substituted and the like, Rrepresents an optionally substituted hydrocarbon group and the like, Rand Rrepresent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol '*' represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein Rand Rare as defined above with a compound represented by the general formula: wherein R, Rand Rare as defined above, and X is a halogen atom.

A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, Ris a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, Ris a hydrogen atom or a lower alkyl group which may be substituted, R, R, R, R, R, Rand Rare independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C-lyase inhibitory activity, and are useful for preventing and treating a mammal suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.

Naphthalene derivatives, their production and use

Process for production of optically active compounds

The present invention provides a compound having a steroid C-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism and tumor such as breast cancer and the like. A compound represented by the formula:wherein R is a hydrogen atom or a protecting group, Ris a lower alkyl group or a cyclic alkyl group, and ring A and ring B are each an optionally substituted 5-membered or 6-membered ring having an amide bond in the ring, or a salt thereof.

Imidazole derivatives, process for their preparation and their use

Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterine myoma, mastopathy and polycystic ovary syndrome are disclosed.

Imidazol-4-ylmehanols and their use as inhibitors of steroid C17-20 lyase

Growing community of inventors

Fukuoka, Japan

Akio Ojida