Chugai Seiyaku Kabushiki Kaisha

Kabushiki Kaisha Toshiba

Denki Kagaku Kogyo Kabushiki Kaisha

Nissan Chemical Industries Limited

Chugai Seikayu Kabushiki Kaisha

Haruhiko Sato

Hiroshi Koga

Takenori Ishizawa

Takuya Shiraishi

Masateru Ohta

Kiyoshi Wagai

Tatsuaki Sekigawa

Hitoshi Yoshino

Hiroyuki Nabata

Mitsuji Shiono

Mitsuaki Nakamura

Kazutaka Tachibana

Etsuro Onuma

Hiromitsu Kawata

Shojiro Kadono

Takashi Dan

Koichi Takahashi

Tadashi Morikawa

Hitoshi Ikeya

Ikuhiro Imaoka

Masahiro Nagamuta

Akie Honma

Tatsuya Tamura

Akira Okamachi

Yoshinobu Higuchi

Shinya Sato

Yoshiaki Watanabe

Takashi Emura

Kazuhiko Ohrai

Masahiro Sakaitani

Yoshiyuki Suzuki

Takanori Shimizu

Keishi Hayashi

Nobuya Ishii

Masami Hasegawa

Masataka Minami

Koji Toyama

Michiaki Adachi

Masayuki Haramura

Toshiro Kozono

Kenji Taniguchi

Noriyuki Izutani

Takaki Koga

Akihisa Sakamoto

Tatsuya Kato

Masakazu Sugiyama

An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted Calkyl group; E is independently selected from a Calkyl group; Rand Rare independently selected from Calkyls; Xand Xare independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is &#x2014;CON(&#x2014;Ra)&#x2014;, &#x2014;CO&#x2014;, &#x2014;OOO&#x2014;, &#x2014;NRa&#x2014;C(&#x2550;NH)NRb&#x2014;, &#x2014;NRa&#x2014;C(&#x2550;N&#x2014;CN)NRb&#x2014;, &#x2014;N(&#x2014;Ra)COO&#x2014;, &#x2014;C(&#x2550;NH)&#x2014;, &#x2014;SO&#x2014;, &#x2014;SON(&#x2014;Ra)&#x2014;, &#x2014;SONR&#x2014;, &#x2014;N(&#x2014;Ra)CO&#x2014;, &#x2014;N(&#x2014;Ra)CON(&#x2014;Rb)&#x2014;, &#x2014;N(COR)CO&#x2014;, &#x2014;N(&#x2014;Ra)SO&#x2014;, &#x2014;N(SOR)SO&#x2014;, &#x2014;N(&#x2014;Ra)&#x2014; or &#x2014;N(&#x2014;Ra)SON(&#x2014;Rb)&#x2014;; Ris independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from Calkyl group, heterocyclic group, aryl group, Ccycloalkyl group and Ccycloalkenyl group; or salt or prodrug thereof.

Imidazolidine derivative and use thereof

An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases. There is provided a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases, wherein methotrexate is conjugated with a carboxyl group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids.

Hyaluronic acid-methotrexate conjugate

The present invention provides novel &#x3b1;-amino acid derivatives of formula (1): (wherein, R, R, R, R, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have &#x3b2;ARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.

&#x3b1;-amino acid derivatives and medicaments containing the same as an active ingredient

An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint disorders. There is provided a hyaluronic acid-methotrexate conjugate useful for the treatment of joint disorders, wherein methotrexate is conjugated with a hydroxy group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids, and the linker is conjugated with the hyaluronic acid through a carbamate group.

The present invention provides a compound represented by formula (I):  A is cyano or the like; B is hydrogen, halogen, or the like; Xand Xare each independently selected from O and S; E is a Calkyl group; and R, R, Rand Rare each independently selected from a hydrogen atom and a C-Calkyl group, and a drug, a pharmaceutical composition containing the compound, and the like.

Imidazolidine derivatives

The present invention provides a compound represented by formula (I): [Formula 1] wherein n is an integer selected from 1 to 20, and Rand R, which may be the same or different, each represent a hydrogen atom, or a linear or branched C-Calkyl group, or a salt, a prodrug or a solvate thereof, as well as a drug, a pharmaceutical composition containing the compound, and the like.

A compound of Formula (1):&#x2003;wherein A crystal of a complex between factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor. A medium carrying a part or all of structure coordinate data of a complex between human factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor, obtainable by X-ray crystal structure analysis of the crystal. A method for computationally designing a low-molecular weight reversible factor VIIa inhibitor using the coordinate data.

Peptide derivatives

Novel benzopyran and benzoxazine derivatives represented by the general formula: wherein R.sub.1 and R.sub.2 represent a lower haloalkyl group, R.sub.3 represents a hydrogen atom, etc., R.sub.4 represents a heterocyclic group or A--O-- wherein A represents a cyclic structure, etc., R.sub.5 and R.sub.6 represent a lower haloalkyl, X represents .dbd.N--, N.fwdarw.O, etc, are disclosed. These compounds exhibit K.sup.+ channel opening activating and can be widely used as an anti-asthma drug, an anti-epilepsy drug, etc.

Benzopyran and benzoxazine derivatives

Novel benzopyran and benzoxazine derivatives represented by the general formula: ##STR1## wherein R.sub.1 and R.sub.2 represent a lower haloalkyl group, R.sub.3 represents a hydrogen atom, etc., R.sub.4 represents a heterocyclic group or A--O-- wherein A represents a cyclic structure, etc., R.sub.5 and R.sub.6 represent a lower haloalkyl, X represents .dbd.N--, N.fwdarw.O, etc, are disclosed. These compounds exhibit K.sup.+ channel opening activating and can be widely used as an anti-asthma drug, an anti-epilepsy drug, etc.

Benzopyran derivatives

N-(2-cyanoethyl)-6-fluoroalkyl-2h-1-benzopyran derivatives

A paging apparatus with a time information generating circuit comprises a combination switch having multiple switch positions in different operation directions, so that a time setting mode is set when a predetermined first operation is performed by the combination switch, and a paging mode is set other operations are performed. When a predetermined second operation is performed with the time setting mode set, time information measured by the time information generating circuit is replaced with time information input by the second operation. Even in the time setting mode, it is checked if a call is made to the apparatus. When there is such a call, a user is informed of this event without ignoring the occurrence of the call.

Paging apparatus equipped with a clock function

A tele-communication device includes a memory for storing a plurality of pieces of messages transmitted over a communication channel and a display device for displaying the message information read from the memory in response to an operation of a display switch. The pieces of message information are automatically read from the memory in sequence at regular intervals and displayed on the display device while the display switch is depressed continuously. When the display time of a message exceeds a given time, the message is automatically erased from the display. When the display switch is depressed within a given time from when the message is erased automatically, the erased message is displayed again.

Radio tele-communication device with received message displaying feature

Novel furobenzisoxazole derivatives of the formula (I): ##STR1## (wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 which may be the same or different represent a hydrogen atom, a halogen atom, or a lower alkyl group having 1-4 carbon atoms; R.sub.5 is a hydroxymethyl group, a carboxyl group or a lower alkoxy carbonyl group having 1-3 carbon atoms; and X is a sulfur atom or a --CH.dbd.CH-- group), as well as intoxic salts thereof when R.sub.5 is a carboxyl group, and process for preparing the same are disclosed. The derivatives of formula (I) and nontoxic salts thereof have hypotensive, uricosuric and diuretic activities and hence ae useful as therapeutics for treating hyperuricemia, edema and hypertension.

Furobenzisoxazole derivatives

Growing community of inventors

Gotenba, Japan

Haruhiko Sato