Shionogi Company Limited

Yoshiharu Hiramatsu

Tsunetoshi Honma

Akinori Arimura

Susumu Mitsumori

Masanao Inagaki

Norihiko Tanimoto

Natsuki Ishizuka

Ikuo Adachi

Jun Sato

Hiroyuki Kai

Hideaki Watanabe

Tetsuo Okada

Akira Kugimiya

Takashi Sasatani

Teruo Yamamori

Hiroshi Hashizume

Satoru Tanaka

Makoto Kakinuma

Motohiko Ueda

Yasuhiko Fujii

Yoshikazu Fukui

Azusa Nozu

Michitaka Shichijo

Ken'ichioh Nakamura

Masahide Odan

Masaru Kawakami

The present invention provides novel compounds having a P2Xand/or P2Xreceptor antagonistic effect, e.g. a compound of Formula (I): wherein wherein

Heterocyclic ring and carbocyclic derivative

The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R, R, R, R, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.

3-carbamoyl-2-pyridone derivatives

The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein Ris optionally substituted C1-C8 alkyl and the like; Ris C1-C6 alkyl; Ris C1-C6 alkyl and the like; or Rand Rtaken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; Ris hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein Ris hydrogen and the like; Xis a single bond and the like; Xis optionally substituted C1-C8 alkylene that may be replaced by one or two groups of &#x2014;O&#x2014;, or &#x2014;N(R)&#x2014;, wherein Ris hydrogen and the like, and the like; Xis a single bond and the like;a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.

The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I)  wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R, R, R, Rand Rare independently a hydrogen atom or a halogen atom etc.; Ris C2-C4 alkyloxy etc.; Ris independently a halogen atom etc.; Ris independently C1-C4 alkyl etc.; Ris carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L, Land Lare a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.

Indole derivative having PGD2 receptor antagonist activity

A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like. A compound of the formula (I): whereina group represented by the formula: is a group represented by the formula: and the like, Ris carboxy and the like, Ris &#x2014;(CH)n-N(&#x2014;Y)&#x2014;SO&#x2014;Ar and the like, the other symbols are as defined in claim

Indole arylsulfonaimide compounds exhibiting PGD 2 receptor antagonism

The present invention provides a process for the preparation of a bicyclic aminoalcohol which comprises reacting a starting compound, nopinone (I), with XCHCOORwherein X is halogen, and Ris alkyl, in the presence of an additive and a base to produce a compound (II), converting it to oxime derivative (III), and reducing it with an aluminum hydride 

Processes for the preparation of bicyclic aminoalcohols

The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin Dreceptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein Ris &#x2014;CH&#x2014;CH&#x2550;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;COORor &#x2014;CH&#x2550;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;COOR; Ris hydrogen or alkyl; m is 0 or 1; p is 0 or 1; Xand Xeach is independently optionally substituted aryl or optionally substituted heteroaryl; Xis a bond, &#x2014;CH&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;CH&#x2014;O&#x2014;, &#x2014;O&#x2014;CH&#x2014;, &#x2014;CH&#x2014;S&#x2014;, &#x2014;S&#x2014;CH&#x2014;, or the like; Xis &#x2014;CH&#x2014;, &#x2014;CH&#x2014;CH&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, or the like, have a dual antagonistic activity against both a thromboxane Areceptor and a prostaglandin Dreceptor.

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Compounds of the general formula (I) which are metabolically stable and have an antagonistic activity against PGDreceptor:&#x2003;wherein Y is bicyclic ring; Ris optionally substituted heteroaryl; Ris hydrogen, etc.; Ris &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2550;CH&#x2014;COOR, &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;X&#x2014;CH&#x2014;COOR, &#x2014;CH&#x2014;CH&#x2550;CH&#x2014;CH&#x2014;X&#x2014;CH&#x2014;COORor &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;COOR; Ris hydrogen, etc.; Xis &#x2014;O&#x2014;, etc.

PGD2 receptor antagonistic pharmaceutical compositions

Processes for producing benzothiophenecarboxylic acid derivatives of the formula (I), which are useful as starting materials for producing drugs, are disclosed. Also disclosed is a process for preparing 5-hydroxybenzo&lsqb;b&rsqb;-thiophene-3-carboxylic acid derivatives of the formula (VI), which are specific PGD antagonists.

Process for preparing 5-hydroxybenzo &lsqb;b&rsqb; thiophene-3-carboxylic acid derivatives

A process for preparing a compound having PGD antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.

Process for preparing benzothiophenecarboxamide derivatives

Process for producing benzothiophenecarboxylic acid amide derivatives

Processes for producing compounds of the formula (VI) are disclosed. Benzothiophenecarboxylic acid derivatives of the formula (I), which are useful as starting materials for producing drugs, are disclosed. Particularly, disclosed is a process for preparing 5-dydroxybenzo&lsqb;b&rsqb;-thiophene-3-carboxylic acid derivatives of the formula (VI), which are specific PGD antagonists are also disclosed.

Benzothiophenecarboxylic acid derivatives of the formula (I) which are useful as starting materials for producing drugs, and a process for preparing 5-hydroxybenzo&lsqb;b&rsqb;-thiophene-3-carboxylic acid derivatives of the formula (VI) which are specific PGD,antagonists.

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Osaka, Japan

Yoshiharu Hiramatsu