Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Masataka Harada

Satoshi Sasaki

Chieko Kitada

Shuji Hinuma

Kazunori Nishi

Nobuhiro Suzuki

Ryo Fujii

Kazuhiro Ogi

Shoichi Ohkubo

Yasuaki Ito

Hideki Kizawa

Masaki Hosoya

Makoto Kobayashi

Yasuaki Itoh

Tsuneo Yasuma

Hideyuki Tanaka

Shuichi Furuya

Nobuo Choh

Yugo Habata

Shoji Fukusumi

Shinobu Sasaki

Yuji Kawamata

Kohji Fukatsu

Hiromi Yoshida

Hidetoshi Komatsu

Yuko Noguchi

The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Receptor function regulator

By using FPRL1 ligand, which comprises the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 17 or SEQ ID NO: 21, and FPRL1, an efficient screening for FPRL1 agonist or FPRL1 antagonist can be performed.

FPRL1 ligands and use thereof

The present invention provides a method of screening a compound or its salt that alters binding properties of a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, and a ligand capable of specifically binding to the protein or its salt, which comprises using (a) the protein, its partial peptide, or a salt thereof and (b) the ligand; a screening kit therefor, and so on. The screening method and kit of the present invention are useful for screening an agent for the prevention/treatment of, e.g., digestive tract disorders, cancer, immune disorders, type II diabetes mellitus or obesity, etc.

Screening method

The present invention provides a method of screening an agonist/antagonist of a G protein-coupled receptor protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or a salt thereof, which comprises using the receptor protein or its salt and a ligand or its salt; and so on. The screening method of the present invention is useful for screening an agent for the prevention/treatment of nervous system diseases or neuropathic pains.

Ligands for G protein-coupled receptor protein and use thereof

The present invention relates to antibodies that bind to the A chain N-terminal peptide. The present invention also relates to (1) a polypeptide containing the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO:7 (A chain), (2) a polypeptide containing the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO:8 (B chain), (3) a polypeptide wherein the A and B chains are bonded to each other via disulfide bonds (2 chains) or its salt., (4) DNAs encoding the same, etc. These polypeptides and DNAs encoding the same can be used for the diagnosis, treatment, prevention, etc. for diseases, including abnormalities (e.g., diabetes mellitus, etc.) in metabolic regulation (sugar metabolism, lipid metabolism, etc.) of energy sources such as carbohydrates.

Antibodies to insulin/IGF/relaxin family polypeptides

By using (1) a G protein-coupled receptor protein having the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1 or its salt and (2) a fatty acid or an eicosanoid, a compound or its salt that can change the binding properties of the receptor protein or its salt to the fatty acid or the eicosanoid can be screened efficiently.

By using a G protein-coupled receptor protein containing an amino acid sequence, which is the same or the substantially the same as an amino acid sequence represented by SEQ ID NO:1, SEQ ID NO:10, SEQ ID NO:12 or SEQ ID NO:14, or its salt together with humanin, a compound or its salt capable of changing the binding properties of the above receptor protein or its salt to humanin can be efficiently screened.

Method of screening therapeutic agents for nerve degeneration associated diseases

The present invention relates to (1) a polypeptide containing the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO:7 (A chain), (2) a polypeptide containing the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO:8 (B chain), (3) a polypeptide wherein the A and B chains are bonded to each other via disulfide bonds (2 chains) or its salt, (4) DNAs encoding the same, etc. These polypeptides and DNAs encoding the same can be used for the diagnosis, treatment, prevention, etc. for diseases, including abnormalities (e.g., diabetes mellitus, etc.) in metabolic regulation (sugar metabolism, lipid metabolism, etc.) of energy sources such as carbohydrates.

Insulin/IGF/relaxin family polypeptides and DNAS thereof

The present thienopyrimidine derivatives and compositions having gonadotropin-releasing hormone antagonistic activity are useful as propylactics or therapeutic agents for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, uterine cervical cancer, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; are effective as a fertility controlling agent in both sexes (e.g. a pregnancy controlling agent and a menstrual cycle controlling agent); can be used as a male or female contraceptive, as an ovulation-inducing agent; can be used as an infertility treating agent by using a rebound effect owing to a stoppage of administration thereof; and are useful for modulating estrous cycles in animals in the field of animal husbandry, as agents for improving the quality of edible meat or promoting the growth of animals; and as agents for promoting spawning in fish.

Thienopyridine compounds which have useful pharmaceutical activity

Growing community of inventors

Tsukuba, Japan

Masataka Harada