Kotobuki Pharmaceutical Co Ltd

Astellas Pharma Gmbh

Kotobuki Pharmaceuticals Co., Ltd.

Hiroshi Tomiyama

Atsushi Noda

Yoshinori Kobayashi

Yoshinori Iwai

Takeshi Murakami

Kazuhiro Ikegai

Masakazu Imamura

Eiji Kurosaki

Kayoko Kitta

Masayuki Yokota

Tsuyoshi Tomiyama

Akio Kamikawa

Takashi Sugane

Ryota Shiraki

Kazuhiko Iikubo

Kazuo Kurosawa

Fumiyoshi Iwasaki

Kozo Miyasaka

Kazuo Tokuzaki

Akira Tomiyama

Itsuro Shimada

Yutaka Kondoh

Yohei Seki

Takahiro Matsuya

Hideyuki Watanabe

Osamu Ikeda

Keiichiro Okuyama

Akihiko Nakamura

Atsushi Suzuki

Takashi Futami

Tomoyuki Suzuki

Takashi Kamikubo

Hiroyuki Moritomo

Takayuki Suzuki

Toshihiro Watanabe

Hiroyuki Hisamichi

Naoto Ueyama

Norio Asai

Jiro Fujiyasu

Ikumi Kuriwaki

Takashi Yanagisawa

Makoto Oku

Motoharu Sonegawa

Takuya Washio

Makoto Asaumi

Kazuhisa Tsunoyama

Akira Ohno

Minoru Kameda

Yukinori Nagakura

Kazumi Kikuchi

Yuichiro Kawamoto

Haruki Okada

Kazuhiro Kosakai

Ryoko Tomita

Masahiro Yanagiya

Yasufumi Ohkura

Masayuki Nimura

Keiko Kuroiwa

A compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody/anti-PD-L1 antibody therapy is provided. The present inventors have conducted studies on a compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody/anti-PD-L1 antibody therapy, and found that a pyridazinyl-thiazolecarboxamide compound has DGK ξ (DGKzeta) inhibitory effect, leading to completion of the present invention. The pyridazinyl-thiazolecarboxamide compound of the present invention has DGK ξ inhibitory effect, and can be used as a therapeutic agent for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody/anti-PD-L1 antibody therapy.

Pyridazinyl-thiazolecarboxamide compound

A compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy is provided. The present inventors have conducted studies on a compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy, and confirmed that a heteroaryl carboxamide compound has DGK ξ (DGKzeta) inhibitory effect, leading to completion of the present invention. The heteroaryl carboxamide compound of the present invention has DGK ξ inhibitory effect, and can be used as a therapeutic agent for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy.

Heteroaryl carboxamide compound

Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.

Diamino heterocyclic carboxamide compound

Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

Nitrogen-containing aromatic heterocyclic compound

The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.

Nitrogen&#x2014;containing heterocyclic derivatives having 2,6-disubstituted styryl

The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via &#x2014;X&#x2014; and A ring is directly bonded to the glucose residue, and it is usable as a Na-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

C-glycoside derivatives and salts thereof

This invention relates to a process for producing optically active alcohols using asymmetric reduction of aromatic ketones. This process gives optically active alcohols in high enantioselectivity in a large scale production.

Process for preparing optically active alcohols

A serum cholesterol lowing agent or a preventive or therapeutile agent for atherosclerosis, which each comprises a combination of a compound represented by the following general formula (I) or pharmaceutical acceptable salts thereof with a cholesterol biosynthesis inhibitor and/or a fibrate type cholesterol lowing agent. (I) (b) (a) [In the formula, A, A, Aand Aeach is hydrogen, a group represented by the formula (b), or a group represented by the formula (a), provided that at least one of these is a group represented by the formula (a); Ais Calkyl etc; and n. p, q and r each is an integer of 0, 1 or 2. 

Serum cholesterol lowering agent or preventative or therapeutic agent for atherosclerosis

This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. wherein: A is selected from &#x2014;(CH)&#x2014;, &#x2014;CO&#x2014;, &#x2014;(CH)&#x2014;CO&#x2014;(CH)&#x2014;, &#x2014;(CH)&#x2014;CS&#x2014;(CH)&#x2014; or a branched alkylene group, B ring and C ring are selected from a benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle compound, D is &#x2014;(CH)&#x2014;, &#x2014;(CH2)&#x2014;O&#x2014;(CH)&#x2014;, &#x2014;(CH)&#x2014;S(O)&#x2014;(CH)&#x2014;, &#x2014;CFor &#x2014;(CH)&#x2014;NR&#x2014;(CH)&#x2014; wherein a D ring is connected with the carbon atom composing the C ring, E is selected from an oxygen atom or a sulfur atom, P is a phosphine atom, R&#x2dc;R, wherein Rand R, Rand Rare joined together with neighbored carbon atom to form 5&#x2dc;7 membered saturated or unsaturated hydrocarbon ring, or 5&#x2dc;6 membered fused heterocycle, R, Rand Rare not a hydrogen atom if the B ring is a benzene ring and may be the same or different and are substituents, Rand Rare may be the same or different and are substituents, Ris an alkyl group, n and m are 0-10 and o is 0-2.

Phosphonic acid derivatives and the treating agents of diseases related hyperphosphatemia

The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

Azulene derivatives and salts thereof

Novel &#x3b2;-lactam compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof which are useful as serum cholesterol-lowering agents: (I) wherein A, Aand Arepresent each hydrogen, halogen Calkyl, Calkoxy, &#x2014;COOR, a group represented by the following general formula (b): (b) wherein Rrepresents hydrogen or Calkyl, or a group represented by the following general formula (a): (a) wherein Rrepresents &#x2014;CHOH, &#x2014;CHOC(O)&#x2014;Ror &#x2014;CO&#x2014;R; Rrepresents &#x2014;OH or &#x2014;OC(O)&#x2014;R; Rrepresents &#x2014;(CH)R(CH)wherein K and 1 are each 0 or an integer of 1 or above provided k+1 is an integer of not more than 10; and Rrepresents a single bond, &#x2014;CH&#x2550;CH&#x2014;, &#x2014;OCH&#x2014;, carbonyl or &#x2014;CH(OH)&#x2014;; provided that at least one of A, Aand Ais a group represented by the above formula (a); Arepresents Calkyl, Calkoxy, Calkenyl, Chydroxyalkyl or Ccarbonylalkyl; and n, p, q and r are each an integer of 0, 1 or 2.

&#x3b2;-lactam compounds process for reproducing the same and serum cholesterol-lowering agents containing the same

An isoquinuclidine derivative represented by the following general formula (I): (I) [wherein Ais methylene or carbonyl]: Ris hydrogen or methyl: Ris &#x2014;(CH)-A-Ph (n is an integer of 0 to 3 and Ais a single bond or &#x2014;O&#x2014;): and Ris &#x2014;COOH, &#x2014;COOR, &#x2014;COSR(Ris lower alkyl, unsubstituted phenyl, or phenyl substituted by a lower alkyl, lower alkoxy, hydroxyl, methoxycarbonyl, ethoxycarbonyl, or trifluoromethanesulfonamide group or by a halogen atom), etc.] or a pharmaceutically acceptable salt of the compound. Also provided is an oral remedy for diabetes, which contains the compound and has hypoglycemic activity.

Isoquinuclidine derivative process for producing the same, and medicinal composition containing the same

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Nagano, Japan

Hiroshi Tomiyama