Astellas Pharma Gmbh

Sekisui Medical Co., Ltd.

Daiichi Sankyo Company, Limited

Daiichi Pharmaceutical Co., Ltd.

Peptidream Inc.

Hideki Kubota

Shinya Yano

Hidenori Azami

Kazunori Kamijo

Masanori Saito

Satoshi Yamamoto

Hirofumi Yamamoto

Masayuki Ito

Ryushi Seo

Kazuyuki Tsuchiya

Takahiro Yamaguchi

Koji Kato

Takeshi Suzuki

Satoru Miyauchi

Hiroyuki Kaizawa

Issei Tsukamoto

Yuta Fukuda

Kenta Saito

Mari Sugita

Takaho Nomura

Kayoko Motoki

Takanori Yasukouchi

Takeshi Fukuda

Hideki Kobayashi

Akira Miyake

Atsushi Hasegawa

Naoki Tanaka

Takashi Tsuji

Toshihiro Mori

Toru Watanabe

Toshio Kaneko

Kenjiro Yamamoto

Hitoshi Yamaguchi

Masanori Miura

Fukushi Hirayama

Tomoyuki Saito

Masaki Abe

Yuji Koga

Keizo Sugasawa

Akihiro Furukawa

Takafumi Shimizu

Patrick Reid

Nobuyuki Ohkawa

Takao Okuda

Shinobu Mochizuki

Yutaka Mori

Ken-Ichi Suzuki

Masami Arai

Shunichiro Matsumoto

Takatoshi Kanayama

Kazuyoshi Obitsu

Ryutaro Wakayama

Shigeo Matsui

Daisuke Takano

Eiichi Nakai

Naoki Terasaka

Hironao Saito

Naoto Katoh

Riki Goto

Koichiro Harada

Susumu Toda

Eri Otsuka

Kiyoshi Yahiro

Kazuhiro Nakatou

Kazuhiro Nakato

Masahiro Ando, Deceased

Toshio Onoda

Takeshi Kuribayashi

Yutaka Ishigai

Kazuki Ono

Hiroshi Ijiri

Hitoshi Iimori

Provided is an alkyldiphenylmethane protective agent, which can prevent solidification or insolubilization of a compound by protecting a functional group of the compound to achieve easy separation and purification after a reaction. An alkyldiphenylmethane compound represented by general formula (1):  

Alkyldiphenylmethane protective agent

An object of the present invention is to develop a protecting group, which can prevent solidification or insolubilization of a compound by protecting a functional group to achieve easy separation and purification after a reaction. A diphenylmethane compound represented by general formula (1):  

Diphenylmethane protective agent

Provided is a compound that can promote angiogenesis by inhibiting the function of TSP1, and is useful for the treatment or prophylaxis of diseases such as critical limb ischemia. Specifically provided is a macrocyclic polypeptide represented by formula (I) [wherein A is selected from the linking groups Ato A; Xis a residue of an aliphatic amino acid, an aromatic amino acid, a basic amino acid, a neutral amino acid, or an acidic amino acid, or is absent; Xis a residue of an aromatic amino acid or a neutral amino acid; Xis a residue of an aliphatic amino acid, an aromatic amino acid, or a basic amino acid; Xis Ser, Thr, Ala, orS; Xis Gly or Ser; Xis a residue of a basic amino acid or a neutral amino acid; Xis a residue of a neutral amino acid or an acidic amino acid; Xis a residue of an aromatic amino acid; Xis a residue of an aliphatic amino acid, a neutral amino acid, or an aromatic amino acid; Xis a residue of a basic amino acid, an aliphatic amino acid, an aromatic amino acid, or a neutral amino acid; Xis a residue of an aromatic amino acid; and Xis a residue of an aliphatic amino acid, an aromatic amino acid, or a basic amino acid], or a pharmacologically acceptable salt thereof.

Thrombospondin 1-binding peptide

The invention is to develop a protecting group that does not solidify or insolubilize a compound in which a functional group has been protected, and facilitates separation and purification after a reaction. Disclosed is a trityl compound represented by General Formula (1): wherein Y represents a hydroxy group or a halogen atom; at least one of Rto Rrepresents a group represented by Formula (2):&#x2014;O&#x2014;R&#x2014;X-A&#x2003;&#x2003;(2)while the other groups each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, or an alkoxy group having 1 to 4 carbon atoms; wherein R, R, and R, which may be identical or different, each represent a linear or branched alkyl group having 1 to 6 carbon atoms, or an aryl group which may have a substituent.

Trityl protecting agent

Provided is an alkyldiphenylmethane protective agent, which can prevent solidification or insolubilization of a compound by protecting a functional group of the compound to achieve easy separation and purification after a reaction. An alkyldiphenylmethane compound represented by general formula (1):   

To develop a protecting group that facilitates separation and purification, after reaction, of a compound including a protected functional group, without solidifying or insolubilizing the compound. A xanthene compound of by General Formula (1)  

Xanthene protective agent

The present invention relates to indole carboxamide compounds of formula (I) or a salt thereof wherein R, R, R, R, R, R, Rand Rhave the meanings as indicated herein, and are MT1 and/or MT2 receptor agonists useful for treating and/or preventing urological diseases.

Indole carboxamide derivative

A compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R is an optionally substituted aryl group or an optionally substituted heteroaryl group. 

Piperidinylpyrazolopyridine derivative

The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by formula (1): [wherein, R: formula (1A): [wherein, Rand R: H, halogen, or alkyl; R: H, halogen, alkyl, or the like; R: substitutable hydroxyalkyl, substitutable hydroxyhalo alkyl, substitutable alkoxyalkyl, or the like; substituent group &#x3b1;: oxo, hydroxy, amino, or the like; ring Q: a monocyclic heterocyclic group; ring Q: a monocyclic hydrocarbon ring group, or a monocyclic heterocyclic group; ring Q: a monocyclic hydrocarbon ring group, or a monocyclic heterocyclic group; X: a single bond, methylene, ethylene, or the like]; R: alkyl, or methylsulfanyl; and R: H, or methyl], or the like.

5-hydroxypyrimidine-4-carboxamide derivative

Substituted imidazo[1,5-a]quinoxalin-4-ones are useful as phosphodiesterase 9 inhibitors.

Substituted imidazo[1,5-a]quinoxalin-4-ones as phosphodiesterase 9 inhibitors

Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones are useful as PDE9 inhibitors.

Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones as PDE9 inhibitors

[Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.

Sulfonamide compounds or salts thereof

The present invention relates to a novel compound having an effect of inhibiting production/secretion of &#x3b2;-amyloid protein. The present invention provides a compound represented by the general formula (1): 

Pyridylmethylsulfone derivative

A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular a lower urinary tract symptom. It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure in which a carbon atom in the amide bonds to the N atom in sulfonamide through lower alkylene, or a salt thereof, has a potent EP1 receptor antagonistic activity, accomplishing the present invention. Since the sulfonamide compound of the present invention or a pharmaceutically acceptable salt thereof has a potent EP1 receptor antagonistic activity, it is useful as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom.

Sulfonamide compound or salt thereof

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Tokyo, Japan

Hideki Kubota