Nof Corporation

Daiichi Pharmaceutical Co., Ltd.

Teruyuki Nagamune

Nagamune, Teruyuki

Chika Itoh

Tohru Yasukohchi

Ken-ichiro Nakamoto

Kazuhiro Kubo

Yuji Yamamoto

Kenji Sakanoue

Syunsuke Ohhashi

Syunsuke Ohashi

Hiroshi Kikuchi

Norio Suzuki

Hitoshi Yamauchi

Miho Takahashi

Tsuyoshi Takehana

Shuichi Yoshimura

Satoshi Matsuo

Kei-ichi Maruyama

Kouzoh Sanchika

Yusuke Ohkawa

Kazuhiro Hashimoto

Miho Kurosawa

Hitoshi Daiichi Pharmaceutical Co Ltd Yamauchi

Miho Daiichi Pharmaceutical Co Ltd Takahashi

Norio Daiichi Pharmaceutical Co Ltd Suzuki

Hiroshi Daiichi Pharmaceutical Co Ltd Kikuchi

Ken-Ichiro Nakamoto

A polyalkylene glycol derivative containing a compound of the formula (1): wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OAand OAare each an oxyalkylene group having 2 to 4 carbon atoms, the groups represented by R are the same or different from each other in one molecule, the groups represented by OAare the same or different from each other in one molecule, m is an average number of moles of the above oxyalkylene group added, m represents 10 to 1000, X represents a functional group capable of chemically reacting with a bio-related substance, and Y is a linker and represents an ether bond, an amide bond, a urethane bond, an ester bond, a secondary amino group, a carbonate bond, or an alkylene group containing these bonds,

Polyalkylene glycol derivative and modified bio-related substance

Provided are a thiol-reactive polyoxyalkylene-modified lipid which can be used to chemically modify bioactive substances and which can be used for drug delivery systems such as liposomes and a method for producing the same. The polyoxyalkylene-modified lipid is represented by the following formula (1): (wherein, Rand Rare hydrocarbon groups which are the same as or different from each other and which contain 4 to 24 carbon atoms, Ris a divalent hydrocarbon group containing 1 to 6 carbon atoms, OA is oxyalkylene groups containing 2 to 4 carbon atoms, n is the average addition mole number of the oxyalkylene groups and is 5 to 1,000, and Z is a group containing either maleimide or iodoacetamide.)

Polyoxyalkylene-modified lipid and method for producing the same

A multibranched polyoxyalkylene compound represented by the following formula (1): wherein Ris the same or different and is a hydrocarbon group having 1 to 24 carbon atoms, OAand OAare the same or different and are an oxyalkylene group having 2 to 4 carbon atoms, n and m are the same or different and are an average number of moles of the oxyalkylene group added, n represents 0 to 1000, m is the same or different and represents 10 to 1000, X represents a functional group capable of reacting with an amino group, a mercapto group, an aldehyde group, a carboxyl group, a triple bond, or an azide group to form a chemical bond, and Land Lare the same or different and are a single bond, an alkylene group, or an alkylene group in which at least one bond selected from an ester bond, a urethane bond, an amide bond, an ether bond, and an amino is interposed.

Multibranched polyoxyalkylene compound and producing method thereof

A process for producing a polyalkylene glycol derivative having such high molecular weight and purity that the derivative can be used in pharmaceutical applications, which produces a polyalkylene glycol derivative of the formula (X) by steps (A), (B), (C) and (D), wherein R is as defined:R&#x2014;(OA)OH&#x2003;&#x2003;(X)

Polyalkylene glycol derivative and process for producing same

A method for producing a polyoxyalkylene derivative represented by the following general formula (1):Z(OA)-OH]&#x2003;&#x2003;(1)wherein Z is a residue of glycerin or diglycerin, OA is an oxyalkylene group having 2 to 4 carbon atoms, n is an average number of moles of the oxyalkylene group added and is 80 to 800, and m is 3 to 4, the method comprising steps (A), (B), (C), (D), (E), and (F) defined in the present description.

Method for producing polyoxyalkylene derivative and polyoxyalkylene derivative

A purification method in which, from a specific polyoxyalkylene derivative having a molecular weight of 8,800 to 100,000, an impurity differing in the number of hydroxyl groups is separated, the method including steps (A), (B), (C), and (D). Step (A): a step in which an aprotic organic solvent is used in an amount at least 5 times by weight the amount of the polyoxyalkylene derivative to dissolve the polyoxyalkylene derivative therein and give a solution; step (B): a step in which an adsorbent comprising an oxide containing at least one of aluminum and silicon is added to the solution in an amount 0.5 to 5 times by weight the amount of the polyoxyalkylene derivative to thereby yield a slurry; step (C): a step in which the slurry is stirred at 25&#xb0; C. or higher; step (D): a step in which the polyoxyalkylene derivative is recovered from the slurry.

Purification method of high-molecular-weight polyoxyalkylene derivative

A modified bio-related substance, wherein at least one poly(alkylene glycol)oxy group represented by the following formula (1) is combined in a molecule: wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OAand OAare each an oxyalkylene group having 2 to 4 carbon atoms, the groups represented by R are the same or different from each other in one molecule, and the groups represented by OAare the same or different from each other in one molecule, n and m are each average number of moles of the oxyalkylene group added, n represents 0 to 1000, and m represents 10 to 1000.

Modified bio-related substance, process for producing the same, and intermediate

A polyalkylene glycol derivative containing a compound of the formula (1): wherein R is a hydrocarbon group having 1 to 24 carbon atoms, OAis an oxyalkylene group having 2 to 4 carbon atoms, the groups represented by R are the same or different from each other in one molecule, the groups represented by OAare the same or different from each other in one molecule, m is an average number of moles of the oxyalkylene group added, m represents 10 to 1000, and X represents a functional group capable of chemically reactive with a bio-related substance,

A phospholipid derivative, utilizable for modification of liposomes and the like, which is a copolymer containing, as essential component units, a component unit A represented by the formula (1), a component unit B represented by the formula (2A) and/or the formula (2B), and a component unit C represented by the formula (3) [Rand Rrepresent hydrogen atom or methyl group, provided that Rand Rdo not simultaneously represent methyl group; Rrepresents a divalent hydrocarbon group having 1 to 3 carbon atoms; AO represents an oxyalkylene group having 2 to 4 carbon atoms; m represents an average molar number of the added oxyalkylene groups and is a number in the range represented as 4&#x2266;m&#x2266;100; Rrepresents hydrogen atom, a hydrocarbon group or acyl group having 1 to 20 carbon atoms; RCO and RCO represent an acyl group having 8 to 24 carbon atoms; Rrepresents a divalent hydrocarbon group having 2 to 4 carbon atoms; and X and Y represent hydrogen atom, an alkali metal atom, ammonium or an organic ammonium] wherein a molar ratio of the component unit A relative to a total of the component unit B and the component unit C is from 7/3 to 3/7, and the component unit C is contained at a ratio of from 1 to 4 moles per 1 mole of the copolymer. 

Phospholipid derivative

A phospholipid derivative represented by the following formula (1): wherein [PG]k represents a residue of polyglycerin having a polymerization degree of k, wherein k is 2 to 50, RCO and RCO independently represent an acyl group having 8 to 22 carbon atoms, symbol 'a' independently represents an integer of 0 to 5, symbol 'b' independently represents 0 or 1, M represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium, and k1, k2, and k3 represent numbers satisfying the following conditions: 1&#x2266;k1&#x2266;(k+2)/2, 0&#x2266;k2, and k1+k2+k3=k+2. The phospholipid derivative is highly safe for living bodies and can be suitably utilized in drug delivery systems such as liposome, and the like.

Phospholipid derivatives and process for the production there

A phospholipid derivative represented by the formula (1) (Z represents a residue of a compound having 3 to 10 hydroxyl groups; AO represents an oxyalkylene group having 2 to 4 carbon atoms; RCO and RCO represent an acyl group having 8 to 22 carbon atoms; X represents hydrogen atom, an alkali metal atom, ammonium or an organic ammonium; 'a' represents an integer of 0 to 4; 'b' represents 0 or 1; Q represents hydrogen atom or methyl group; m represents an average number of moles of the oxyalkylene group added; and m, k1, k2, and k3 are numbers satisfying the following conditions: 3&#x2266;m&#x2266;200, 9&#x2266;m&#xd7;(k1+k2+k3)&#x2266;1000, 1&#x2266;k1&#x2266;2, 0&#x2266;k2&#x2266;9 and 0&#x2266;k3&#x2266;9, and 3&#x2266;k1+k2+k3&#x2266;10), which is highly safe for living bodies, and is suitably used for solubilization and dispersion of physiologically active substances and the like, or in the fields of drug delivery systems such as liposomes and cosmetics. 

A phospholipid derivative represented by the following formula (I) wherein RCO and RCO independently represent an acyl group; Rrepresents hydrogen atom, or a hydrocarbon group; symbol 'a' represents an integer of 0 to 4; symbol 'b' represents 0 or 1, provided that when a is 0, b is 0; X represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium; AO and AO represent an oxyalkylene group containing oxyethylene group, wherein the ratio of the oxyethylene group to the oxyalkylene group in AO and AO is 0.5 or larger in terms of a weight ratio; AO represents an oxyalkylene group; symbols &#x201c;m&#x201d; and &#x201c;q&#x201d; represent an average molar number of added oxyalkylene groups; and symbol &#x201c;n&#x201d; represent an average molar number of added oxyalkylene groups; provided that m, n and q satisfy the following conditions: 5&#x2266;m&#x2266;600, 1&#x2266;n&#x2266;45, 0&#x2266;q&#x2266;200, 10&#x2266;m+n+q&#x2266;600, 0.04&#x2266;n/(m+n+q), and q/(m+n+q)&#x2266;0.8, which can thicken the water shell of liposome surface by suppressing the spreading of the polyalkylene oxide structure on the surface and thus increase stability of the liposome 

A cell in which a reaction product of a substance to be modified and an amphipathic compound is non-covalently bound to a cell membrane, wherein said compound has the following features:

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Kanagawa, Japan

Chika Itoh