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    GIP RECEPTOR AGONIST PEPTIDE COMPOUNDS AND USES THEREOF
    1.
    发明申请
    GIP RECEPTOR AGONIST PEPTIDE COMPOUNDS AND USES THEREOF 审中-公开

    公开(公告)号：WO2020067557A2

    公开(公告)日：2020-04-02

    申请号：PCT/JP2019/038441

    申请日：2019-09-24

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： IMOTO, Hiroshi ,  ADACHI, Mari ,  KANEMATSU, Yoko ,  ASAMI, Taiji ,  NIIDA, Ayumu ,  NISHIZAWA, Naoki ,  COLE, Derek, Cecil ,  FLINSPACH, Mack ,  SCORAH, Nick ,  BHAT, Abhijit, Suresh

    Abstract: The present disclosure provides GIP receptor agonist peptide compounds having an activating action on GIP receptors and use of the GIP receptor agonist peptide as a medicament for the treatment and/or prevention of diabetes, obesity, emesis, or a symptom or condition associated with diabetes, obesity, or emesis. Specifically, a GIP receptor agonist peptide containing a sequence represented by the formula (I) or a salt thereof, and a medicament comprising the same are provided. Formula I: P 1 - A 1 - A2- A3 - A4- A5 - A6- A7 - A8-A9-A 10- A 11 - A 12- A 13- A 14- A 15-A 16-A 17-A18-A19-A20-A21 -A22-A23-A24-A25- A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-A37-A38-A39-A40-A41-P2 (SEQ ID NO: 4), or a salt thereof, wherein each symbol is as defined herein, with the proviso that the GIP receptor agonist peptide does not have an amino acid sequence as provided in SEQ ID NOs: 4-569 disclosed in PCT/JP2018/013540.

    PROCESS FOR PRODUCING OPTICALLY ACTIVE SULFOXIDE DERIVATIVE
    3.
    发明公开
    PROCESS FOR PRODUCING OPTICALLY ACTIVE SULFOXIDE DERIVATIVE 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES OPTISCH AKTIVEN SULFOXID DERIVATS

    公开(公告)号：EP1484322A1

    公开(公告)日：2004-12-08

    申请号：EP03708541.2

    申请日：2003-03-11

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： TAWADA, Hiroyuki ,  IKEMOTO, Tomomi ,  NISHIGUCHI, Atsuko ,  ITO, Tatsuya, 117.1-7 Asahigaoka-Kukakuseirichinai ,  ADACHI, Mari

    IPC: C07D233/64 ,  C07D403/12 ,  A61K31/4164 ,  A61K31/55 ,  A61K31/4178 ,  A61P43/00

    CPC classification number: C07D233/64 ,  C07D225/06 ,  C07D403/12 ,  Y02P20/582

    Abstract: A process for preparing an optically active sulfoxide derivative (I) having CCR5 antagonism without causing side reactions such as racemization and Pummerer rearrangement, which comprises reacting a compound (II) with a compound (III) as shown by the following scheme:
    wherein R 1 represents hydrogen, an aliphatic hydrocarbon group or an aromatic group; R 2 represents halogeno, alkyl, hydroxyl, amino, an aromatic group, etc.; R 3 represents a 5- or 6-membered ring; R 4 represents hydrogen, alkyl, alkoxy or halogeno; R 5 represents hydrogen, a hydrocarbon group, a heterocyclic group, acyl, etc.; ring A represents an optionally substituted benzene ring; X represents a bond or divalent group comprising a linear part constituted of 1 to 4 atoms; m represents an integer of 1 to 5; n represents an integer of 0 to 3; p represents an integer of 0 to 2; and *1 represents an asymmetric center.

    Abstract translation: 一种制备具有CCR5拮抗作用的光学活性亚砜衍生物（I）的方法，其不引起外消旋和Pummerer重排的副反应，其包括使化合物（II）与化合物（III）反应，如下列方案所示： 其中R 1表示氢，脂族烃基或芳基; R 2表示卤代，烷基，羟基，氨基，芳基等; R 3表示5-或6-元环; R 4表示氢，烷基，烷氧基或卤代; R 5表示氢，烃基，杂环基，酰基等; 环A表示任选取代的苯环; X表示包含由1至4个原子构成的直链部分的键或二价基团; m表示1〜5的整数， n表示0〜3的整数， p表示0〜2的整数， 并且<* 1>表示不对称中心。

    PROCESS FOR PRODUCING OPTICALLY ACTIVE NAPHTHALENE DERIVATIVE AND OPTICAL RESOLVER THEREFOR
    4.
    发明授权
    PROCESS FOR PRODUCING OPTICALLY ACTIVE NAPHTHALENE DERIVATIVE AND OPTICAL RESOLVER THEREFOR 有权
    工艺制备光学活性萘及其使用的光学RESOLVER

    公开(公告)号：EP1227085B1

    公开(公告)日：2006-03-15

    申请号：EP00969902.6

    申请日：2000-10-19

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： AOKI, Isao ,  ADACHI, Mari ,  KAWADA, Mitsuru ,  YAMANO, Toru ,  TAYA, Naohiro

    IPC: C07D233/64 ,  C07F9/6574 ,  C07C57/00 ,  C07D233/54

    CPC classification number: C07D233/64 ,  A61K31/4164 ,  C07B2200/07 ,  C07F9/5027 ,  C07F9/65744

    Abstract: A process for producing an optically active isomer of a compound represented by formula (I) which comprises: reacting a mixture of naphthalene derivatives represented by formula (I) (wherein R represents a nitrogenous heterocyclic group; R1 represents hydrogen, a hydrocarbon group, or a mononuclear aromatic heterocyclic group; R2 represents hydrogen or lower alkyl; symbol * indicates the position of an asymmetric carbon atom; and R3 to R8 each represents hydrogen, a hydrocarbon group, hydroxy, etc., provided that R7 may be bonded to R6 or R8 to form a ring containing an oxygen atom) with an optically active isomer of a compound represented by formula (II) or (III) (wherein ring A represents a benzene ring; R?10 and R11¿ each represents hydrogen, a hydrocarbon group, etc. or R?10 and R11¿ in combination represent alkylene; symbol * indicates the position of an asymmetric carbon atom; and rings B and C each represents an aromatic ring) to yield salts; separating the salts; and then isolating the target isomer. The optically active isomer produced has a steroid C¿17,20? lyase inhibitory activity and is useful as a preventive/remedy for tumors such as prostatism and mammary cancer. Also provided is a novel optical resolver.

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