Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Other

Nkk Corporation

Takasago International Corporation

Japan Science and Technology Corporation

Research Development Corporation of Japan

Asahi Kasei Pharma Corporation

Shohei Hashiguchi

Masanori Baba

Naoyuki Kanzaki

Osamu Nishimura

Takao Ikariya

Shinichi Imamura

Yuji Iizawa

Tomoyasu Ishikawa

Akio Fujii

Ryoji Noyori

Kazuhiko Matsumura

Jun Takehara

Yoshihiro Sugihara

Taeko Hattori

Nobuyuki Uematsu

Mitsuru Shiraishi

Tomohiro Kaku

Akihiro Tasaka

Takeshi Ohkuma

Masami Kusaka

Osamu Kurasawa

Nobuo Seido

Toshifumi Watanabe

Masuo Yamaoka

Yoshi Nara

Noritaka Kuroda

Hirohito Ooka

A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CHCOOH, CHCHCOOH or CHCN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like. 

Phosphonocephem compound

A compound of formula (I) (wherein Ris a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, Ris a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or Rand Rmay combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N&#x2014;R.Y(Ris a hydrocarbon group; Yis a counter anion); Ris a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; Ris a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; Gis a bond, CO or SO; Gis CO, SO, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent Caliphatic hydrocarbon which may be substituted; provided that J is methine when Gis OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when Gis a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).

Cyclic amine compounds as CCR5 antagonists

The present invention provides a pharmaceutical composition having a steroid C-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C-lyase inhibitor containing a compound represented by the formula: wherein Ais an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of Aand Ais a hydrogen atom, a halogen atom, a Caliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of Aand Ais an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A, Aand Ais a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.

Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparing the same and use thereof

A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CHCOOH, CHCHCOOH or CHCN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.

A method for producing optically active compounds is disclosed. The method is highly practical for producing optically active compounds useful for various utilities such as intermediates for synthesizing pharmaceutical agents, liquid crystal materials and agents for optical resolution.

Method for producing optically active compounds

Urea compounds, process for producing the same and use thereof

A compound of formula (I) (wherein R is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R and R may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N &mdash;R .Y (R is a hydrocarbon group; Y is a counter anion); R is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G is a bond, CO or SO ; G is CO, SO , NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C aliphatic hydrocarbon which may be substituted; provided that J is methine when G is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).

Phosphonocephem derivatives, process for the preparation of the same, and use thereof

This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various applications, for example, as synthetic intermediates of pharmaceuticals, liquid crystal materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compounds as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound.

Process for preparing optically active compounds

The present invention provides a method for producing a alcohol including an optically active alcohol by hydrogenating a carbonyl compound in the presence of a homogeneous catalyst, a base and a nitrogen-containing organic compound. Thus, the reaction employs an inexpensive catalyst and proceeds in high yield and high efficiency.

Method for producing an alcohol

A new compound of the formula: ##STR1## wherein ##STR2## is an optionally substituted benzene ring; R.sup.1 is a carbocyclic or heterocyclic group which is linked to the 4-position of the 1,3-benzoxazine ring through a carbon-carbon bond, a hydrocarbon residue, etc.; and R.sup.2 and R.sup.3 are independently a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group, etc., or a salt thereof is useful for treating and preventing heart, circulatory, respiratory and cerebral diseases.

1,3-benzoxazine derivatives, their production and use

Growing community of inventors

Toyonaka, Japan

Shohei Hashiguchi