Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Prism Pharma Co., Ltd.

Yuji Yamamoto

Akihiko Tsuruoka

Yasuhiro Funahashi

Keiko Takahashi

Toru Haneda

Junichi Kamata

Norihiro Ueda

Tadashi Okabe

Kazumasa Nara

Takashi Owa

Taro Semba

Shinichi Hamaoka

Toshiaki Wakabayashi

Naoko Hata

Tatsuo Watanabe

Junji Matsui

Yoichi Ozawa

Tomohiro Matsushima

Hiroshi Obaishi

Noako Tsukahara

Masayuki Matsukura

Kazuki Miyazaki

Yoshio Fukuda

Toshimitsu Uenaka

Atsumi Yamaguchi

Takayuki Nakagawa

Katsuji Nakamura

Ken-ichi Nomoto

Sachi Suzuki

Fusayo Mimura

Satoshi Inoue

Yasuyuki Suzuki

Kenichi Nomoto

Naoko Tsukahara

Itaru Arimoto

Saori Miyano

Takako Yoshiba

Kentaro Iso

Masayuki Okada

Kenji Matsui

The present application discloses a therapeutic agent for breast cancer, comprising 5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamide)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide or a pharmacologically acceptable salt thereof.

Therapeutic agent for breast cancer

A compound represented by formula (1) or pharmaceutically acceptable salt thereof: wherein Ris a Calkyl group; Rand Rare the same or different from each other and each is a hydrogen atom or a Calkyl group; X, Xand Xare the same or different from each other and each is a hydrogen atom or a halogen atom; and Xis a hydrogen atom or &#x2014;P(&#x2550;O)(OH)has a Wnt Pathway modulating activity.

(6S,9aS)-N-benzyl-6-[(4-hydroxyphenyl)methyl]-4,7-dioxo-8-({6-[3-(piperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-2-(prop-2-en-1-yl)-octahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide compound

The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.

Method for assay on the effect of vascularization inhibitor

The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EOF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.

Disclosed are: a therapeutic agent, a kit and a treatment method for undifferentiated gastric cancer; and a pharmaceutical composition, a kit and a treatment method which are more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. A combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on undifferentiated gastric cancer. The combination of a FGFR2 inhibitor and a therapeutic substance for gastric cancer is more effective on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR2 and a cell expressing a mutant FGFR2. 

Composition for treatment of undifferentiated gastric cancer

The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy- 6 quinolinecarboxamide or an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with an anti-tumor platinum complex.

Combination of anti-angiogenic substance and anti-tumor platinum complex

The present invention relates to a therapeutic agent represented by the General formula (I), or a pharmacologically acceptable salt thereof, or a solvate of the compound or the salt thereof:  The therapeutic agent comprises a substance having the activity of inhibiting kinase activity of fibroblast growth factor receptor 2 ('FGFR2'). The therapeutic agent can be used for treating undifferentiated gastric cancer, and can also be used to treat organisms comprising a cell overexpressing FGFR2 or a cell expressing mutant FGFR2, or both. The present invention further relates to a pharmaceutical composition comprising an FGFR2 inhibitory and methods of treatment therewith. The present invention also relates to a method for predicting the effect of an FGFR2 inhibitory substance on a patient.

Antitumor agent for undifferentiated gastric cancer

The object of the present invention is to find a pharmaceutical composition and a method for treating cancer that show an excellent antitumor effect. Combinational use of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and analogues thereof can result in an excellent antitumor effect when combined with a substance having a c-kit kinase-inhibiting activity.

Use of combination of anti-angiogenic substance and c-kit kinase inhibitor

It was discovered that a compound represented by the general formula (I) shows strong c-Kit kinase inhibitory activity, and it inhibits proliferation of c-Kit kinase activated-cancer cells in vitro and in vivo. A novel anticancer agent showing c-Kit kinase inhibitory activity was discovered. The general formula (I): (wherein Rrepresents methyl etc., Rrepresents cyano etc., Rrepresents hydrogen etc., Rrepresents hydrogen etc.).

c-Kit kinase inhibitor

The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, wherein in the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, &#x2014;CH&#x2550;CH&#x2014; or &#x2014;(CRR)&#x2014; (wherein Rand Rare the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mmeans an integer of 1 or 2); Rmeans hydrogen atom or a C1-C6 alkyl group; Z means a single bond or &#x2014;CO&#x2014;NH&#x2014;; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

Integrin expression inhibitor

Compounds represented by the following general formula: [wherein Ais an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xis &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Yis an optionally substituted Caryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tis a group represented by the following general formula: (wherein Eis a single bond or &#x2014;N(R)&#x2014;, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, etc. and Zrepresents a Calkyl group, a Calicyclic hydrocarbon group, a Caryl group, etc.)], salts thereof or hydrates of the foregoing.

Nitrogen-containing aromatic derivatives

Compounds represented by the following general formula: [wherein Ais an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xis &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Yis an optionally substituted Caryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tis a group represented by the following general formula: (wherein Eis a single bond or &#x2014;N(R)&#x2014;, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, etc. and Zrepresents a Calkyl group, a Calicyclic hydrocarbon group, a Caryl group, etc.)],

Sulfonamide-containing heterocyclic compounds

Sulfonamide-containing indole compounds

A method for producing a cell to which angiogenesis-inducing ability has been imparted, comprising the steps of introducing a gene of an angiogenic factor into a human or animal cell having low angiogenesis-inducing ability, and selecting a cell that overexpresses the angiogenic factor; and a method for screening for an angiogenesis inhibitor or a substance having anticancer activity by using the produced cell.

Human cancer cell line malignantly altered by expression of angiogenic factor

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Tsukuba, Japan

Yuji Yamamoto