Takeda Chemical Industries, Inc.

Tokyo Metropolitan Institute for Neurosciences

Yoshio Aramaki

Mitsuru Shiraishi

Masanori Baba

Naoyuki Kanzaki

Osamu Nishimura

Tsuneo Oda

Susumu Honda

Takahito Kitayoshi

Hidekazu Sawada

Ken-ichi Kuroshima

Masaki Seto

Hirotomo Masuya

Yuji Iizawa

Naoki Miyamoto

Terumi Nakajima

Nobufumi Kawai

Masanori Yoshioka

Tsutomu Higashijima

Akiko Miwa

Tadashi Yasuhara

The present invention provides a novel benzazepine derivative represented by formula: wherein, Ris a 5- or 6-membered aromatic ring, Ris lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula &#x2014;W&#x2014;X&#x2014;W&#x2014; (Wand Ware independently S(O)(m1 is 0, 1, or 2), etc., and Xis an optionally substituted alkylene group etc.), a preparation method and use thereof.

Benzazepine derivative, process for producing the same, and use

Compounds of the general formula (I):or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein Ris a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z-X-Z- (wherein Ris hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Zand Zare each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and Rand Rare each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.

Benzazepine derivatives, process for the preparation of the same and uses thereof

Anilide derivative, production and use thereof

Quaternary ammonium salts and their use

This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula:

Pharmaceutical composition for antagonizing CCR5 comprising anilide derivative

This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.

This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: ##STR1## wherein R.sup.1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is --CH.sub.2 --, --S-- or --O--; and R.sup.2, R.sup.3 and R.sup.4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.

An assay method which comprises utilizing chemiluminescence of a pyridopyridazine compound of the formula ##STR1## wherein R.sub.1 is a hydrocarbon group or a heterocyclic group each of which may be substituted and R.sub.2 is hydroxy group, thiol group, amino group or a monosubstituted amino group, and when R.sub.2 is a monosubstituted amino group, R.sub.2 may be taken together with R.sub.1 to form the ring; R.sub.3 is hydrogen atom, a hydroxy group which may be substituted, an amino group which may be substituted, a thiol group which may be substituted, a halogen atom, a heterocyclic group, nitro group, cyano group, carboxyl group which may be esterified or amidated, azido group, sulfo group or an organic sulfonyl group, provided that when R.sub.1 is an aliphalic group, R.sub.3 is not hydrogen atom; and X is oxygen atom or sulfur atom/or a salt thereof; and a novel compound of the formula (I) wherein the symbols are as defined above with proviso that R.sub.3 is hydrogen atom, R.sub.1 is a substituted aryl group or a heterocyclic group which may be substituted, or a salt thereof and the production methods thereof.

Pyridopyridazine compounds and their use

A compound having glutamate receptor inhibitor activity represented by the formula: ##STR1## where R represents a hydrogen atom or a group of the formula: ##STR2## m and n each represents an integer of 3 or 4 and p represents an integer of 0 or 1, or a salt thereof is provided. The compounds are useful for an insecticide.

Glutamate receptor inhibitor

Growing community of inventors

Osaka, Japan

Yoshio Aramaki